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  • Structure-Activity Relationship  (85)
  • American Association for the Advancement of Science (AAAS)  (85)
  • Annual Reviews
  • 1980-1984  (85)
Collection
Keywords
Publisher
  • American Association for the Advancement of Science (AAAS)  (85)
  • Annual Reviews
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Year
  • 1
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    Bioactive conformation of luteinizing hormone-releasing hormone: evidence from a conformationally constrained analog (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-11-07
    Description: An analog of luteinizing hormone-releasing hormone containing a gamma-lactam as a conformational constraint has been prepared with the use of a novel cyclization of a methionine sulfonium salt. The analog is more active as a luteinizing hormone-releasing hormone agonist that the parent hormone, and provides evidence for a bioactive conformation containing a beta-turn.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Freidinger, R M -- Veber, D F -- Perlow, D S -- Brooks, J R -- Saperstein, R -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):656-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7001627" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Biological Assay ; Cells, Cultured ; Female ; *Gonadotropin-Releasing Hormone/analogs & derivatives ; Hydrogen Bonding ; Lactams ; Protein Conformation ; Rats ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 2
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    Three-dimensional molecular modeling and drug design (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-06-27
    Description: A discussion of drug-receptor theory is used to show that the three-dimensional structure, or shape, of molecules is important for biological activity. The computer-assisted molecular modeling system at Merck is described, and it is shown that this system is useful for generating and storing molecular structures, determining preferred conformation, comparing molecular shapes, and computing molecular properties. Applications of the system to the study of anti-inflammatory drugs, somatostatin-like compounds, and dihydrofolate reductase inhibitors are summarized.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gund, P -- Andose, J D -- Rhodes, J B -- Smith, G M -- New York, N.Y. -- Science. 1980 Jun 27;208(4451):1425-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6104357" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arachidonic Acids ; Binding Sites ; Computers ; Cyclooxygenase Inhibitors ; Humans ; Indomethacin ; *Models, Molecular ; *Models, Structural ; *Molecular Conformation ; *Pharmaceutical Preparations ; Receptors, Drug/metabolism ; Somatostatin/analogs & derivatives ; Structure-Activity Relationship
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 3
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    Vesicle targeting: timed release and specificity for leukocytes in mice by subcutaneous injection (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-01-18
    Description: When unilamellar vesicles were administered subcutaneously in mice, the half-time for the destruction of the vesicles varied from 12 to 600 hours, depending on their composition. The vesicles tested consisted of distearoyl phosphatidylcholine, cholesterol, and certain sugar and amino-sugar derivatives of cholesterol. Vesicle with amino-sugar derivatives showed the greatest longevity and became localized with high specificity in aggregates of polymorphonuclear leukocytes. A substantial delay between the time that the vesicles broke open and the time that labels contained in the vesicles were excreted suggests that the vesicles undergo endocytosis before destruction.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Mauk, M R -- Gamble, R C -- Baldeschwieler, J D -- New York, N.Y. -- Science. 1980 Jan 18;207(4428):309-11.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7350660" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cholesterol/analogs & derivatives ; Endocytosis ; Liposomes/*therapeutic use ; Lysosomes/metabolism ; Metabolic Clearance Rate ; Mice ; Neutrophils/*metabolism ; Phosphatidylcholines ; Structure-Activity Relationship
    Print ISSN: 0036-8075
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  • 4
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    Regression of tumors in guinea pigs after treatment with synthetic muramyl dipeptides and trehalose dimycolate (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-04-25
    Description: A high incidence of tumor regression was observed in guinea pigs bearing transplantable, line-10 hepatocellular carcinomas when synthetic muramyl dipeptides combined with trehalose dimycolate in oil-in-water emulsions were injected directly into the tumors. These compounds are promising candidates to replace viable bacillus Calmette-Guerin in cancer immunotherapy in humans and animals.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉McLaughlin, C A -- Schwartzman, S M -- Horner, B L -- Jones, G H -- Moffatt, J G -- Nestor, J J Jr -- Tegg, D -- New York, N.Y. -- Science. 1980 Apr 25;208(4442):415-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7189295" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylmuramyl-Alanyl-Isoglutamine/administration & dosage/*therapeutic use ; Animals ; Cord Factors/administration & dosage/*therapeutic use ; Drug Combinations ; Emulsions ; Glycolipids/*therapeutic use ; Glycopeptides/*therapeutic use ; Immunotherapy ; Liver Neoplasms, Experimental/*therapy ; Lymphatic Metastasis ; Structure-Activity Relationship
    Print ISSN: 0036-8075
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 5
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    Stereospecific nicotine receptors on rat brain membranes (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-11-07
    Description: A stereospecific binding site for nicotine has been detected on rat brain membranes. Competition studies with cholinergic agonists suggest that this site is a nicotinic cholinergic receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Romano, C -- Goldstein, A -- DA-1938/DA/NIDA NIH HHS/ -- DA-7063/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):647-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7433991" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Binding, Competitive ; Brain/*metabolism ; Ligands ; Male ; Nicotine/metabolism ; Rats ; Receptors, Cholinergic/*metabolism ; Receptors, Nicotinic/*metabolism ; Stereoisomerism ; Structure-Activity Relationship ; Synaptic Membranes/metabolism
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 6
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    GABA analogues activate channels of different duration on cultured mouse spinal neurons (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-04-17
    Description: Voltage-clamp recordings from mouse spinal neurons grown in culture were used to study the membrane current fluctuations induced by 12 substances structurally similar to gamma-aminobutyric acid (GABA). Fluctuation analysis provided estimates of the electrical properties of the elementary events underlying these responses. Estimates of the mean conductance of channels activated by all of the substances except glycine did not differ significantly from that estimated for GABA, whereas mean durations of agonist-activated channels all differed significantly from that found for GABA. The results indicate that all of the substances tested except glycine activate channels of similar conductance but of different durations.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Barker, J L -- Mathers, D A -- New York, N.Y. -- Science. 1981 Apr 17;212(4492):358-61.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6259733" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Membrane/drug effects ; Ion Channels/*drug effects ; Membrane Potentials/drug effects ; Mice ; Neurons/drug effects ; Receptors, Cell Surface/metabolism ; Receptors, GABA-A ; Spinal Nerves/*drug effects ; Structure-Activity Relationship ; Time Factors ; gamma-Aminobutyric Acid/*analogs & derivatives/pharmacology
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  • 7
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    Multiple opiate receptors: alcohol selectively inhibits binding to delta receptors (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-10-23
    Description: The addition of ethanol or other aliphatic alcohols to rat brain membranes strongly inhibits binding of enkephalins at concentrations at which little inhibition of opiate alkaloids is seen. Inhibition is reversible, and potency increases with chain length of the alcohol. The results suggest that delta receptors are considerably more sensitive to alcohols than mu receptors. This is the first demonstration of selective inhibition of one of the postulated classes of opiate receptors by a reagent that is not a ligand for the receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hiller, J M -- Angel, L M -- Simon, E J -- DA-00017/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1981 Oct 23;214(4519):468-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6270788" target="_blank"〉PubMed〈/a〉
    Keywords: Alcohols/*pharmacology ; Animals ; Brain/metabolism ; Cells, Cultured ; In Vitro Techniques ; Neuroblastoma/metabolism ; Rats ; Receptors, Opioid/classification/*drug effects/metabolism ; Structure-Activity Relationship
    Print ISSN: 0036-8075
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  • 8
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    Insulin as a potent, specific growth factor in a rat hepatoma cell line (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-02-27
    Description: A line or rat hepatoma cells in culture which, in response to serum starvation, become arrested in the early G1 phase of growth, can be stimulated by insulin alone to enter the cell cycle and traverse S phase. A half-maximum response is observed at 30 to 70 picomolar concentrations and the maximum response is essentially identical to that found with optimum serum concentrations.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Koontz, J W -- Iwahashi, M -- AM 24047/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Feb 27;211(4485):947-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7008195" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Cycle/drug effects ; Cell Division/drug effects ; Cell Line ; *Growth Substances ; Insulin/*pharmacology ; Liver Neoplasms, Experimental/*pathology ; Mitosis/drug effects ; Proinsulin/pharmacology ; Rats ; Structure-Activity Relationship
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  • 9
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    Rational approaches to chemotherapy: antisickling agents (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-08-14
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Klotz, I M -- Haney, D N -- King, L C -- New York, N.Y. -- Science. 1981 Aug 14;213(4509):724-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7256275" target="_blank"〉PubMed〈/a〉
    Keywords: Anemia, Sickle Cell/*drug therapy ; Aspirin/analogs & derivatives/therapeutic use ; Chemical Phenomena ; Chemistry ; *Hemoglobin, Sickle ; Humans ; Protein Binding/drug effects ; Protein Conformation ; Salicylates/*therapeutic use ; Solubility ; Structure-Activity Relationship
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 10
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    Asbestos surface charge heterogeneity and biological effects (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-25
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Light, W G -- New York, N.Y. -- Science. 1981 Sep 25;213(4515):1534.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7280676" target="_blank"〉PubMed〈/a〉
    Keywords: *Asbestos ; Humans ; Occupational Diseases/chemically induced ; Structure-Activity Relationship
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  • 11
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    Growth inhibition by adenosine 3',5-monophosphate derivatives does not require 3',5' phosphodiester linkage (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-04
    Description: Analogs of adenosine 3',5'-monophosphate (cyclic AMP) inhibit the growth of cultured cell lines. The effects of 8-bromo- and N6-butyryl-substituted analogs of cyclic and noncyclic AMP on six cell lines were examined and were equally inhibitory. Variant cell lines with altered cyclic AMP-dependent protein kinase were more resistant to both cyclic and noncyclic nucleotides. We conclude that growth inhibition by analogs of cyclic AMP (i) does not require a 3',5' phosphodiester bond and (ii) may be mediated by a pathway involving endogenous cyclic AMP.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Martin, T F -- Kowalchyk, J A -- AM 25861/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 4;213(4512):1120-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6267695" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Division/*drug effects ; Cell Line ; Cricetinae ; Cyclic AMP/*pharmacology ; DNA/biosynthesis ; Growth Inhibitors/*pharmacology ; Mice ; Phosphodiesterase Inhibitors/pharmacology ; Structure-Activity Relationship
    Print ISSN: 0036-8075
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  • 12
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    A new wave of antibiotics builds (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-12-11
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H -- New York, N.Y. -- Science. 1981 Dec 11;214(4526):1225-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7302591" target="_blank"〉PubMed〈/a〉
    Keywords: *Cephalosporins/therapeutic use ; Humans ; Research ; Structure-Activity Relationship ; United States
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  • 13
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    Thymosin stimulates secretion of luteinizing hormone-releasing factor (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-11-06
    Description: Partially purified thymosin fraction 5 and one of its synthetic peptide components, thymosin beta 4, but not thymosin alpha 1, stimulated secretion of luteinizing hormone--releasing factor from superfused medial basal hypothalami from random cycling female rats. In addition, luteinizing hormone was released from pituitary glands superfused in sequence with hypothalami. No release of luteinizing hormone in response to thymosin was observed from pituitaries superfused alone. These data provide the first evidence of a direct effect of the endocrine thymus on the hypothalamus and suggest a potentially important role for thymic peptides in reproductive function.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rebar, R W -- Miyake, A -- Low, T L -- Goldstein, A L -- AG-01531/AG/NIA NIH HHS/ -- HD-12303/HD/NICHD NIH HHS/ -- HD-14362/HD/NICHD NIH HHS/ -- etc. -- New York, N.Y. -- Science. 1981 Nov 6;214(4521):669-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7027442" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Gonadotropin-Releasing Hormone/*secretion ; Hormones/pharmacology ; Hypothalamo-Hypophyseal System/drug effects ; Hypothalamus/*drug effects ; Peptide Fragments/pharmacology ; Rats ; Structure-Activity Relationship ; Thymosin/*pharmacology ; Thymus Hormones/*pharmacology
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  • 14
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    Didemnins: antiviral and antitumor depsipeptides from a caribbean tunicate (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-05-22
    Description: Extracts of samples of a Caribbean tunicate (ascidian, sea squirt) of the family Didemnidae inhibit in vitro at low concentrations the growth of DNA and RNA viruses as well as L1210 leukemic cells. The active compounds isolated from the tunicate, didemnins A, B, and C, are depsipeptides, and didemnin B (a derivative of didemnin A) is the component active at the lowest concentration in inhibiting viral replication in vitro and P388 leukemia in vivo.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rinehart, K L Jr -- Gloer, J B -- Hughes, R G Jr -- Renis, H E -- McGovren, J P -- Swynenberg, E B -- Stringfellow, D A -- Kuentzel, S L -- Li, L H -- AI 04769/AI/NIAID NIH HHS/ -- GM 27029/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1981 May 22;212(4497):933-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233187" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Antibiotics, Antineoplastic/*isolation & purification ; Antiviral Agents/*isolation & purification ; *Depsipeptides ; Leukemia, Experimental/*drug therapy ; Peptides, Cyclic/*isolation & purification/therapeutic use ; Structure-Activity Relationship ; Urochordata/*analysis
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  • 15
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    Micromolar affinity benzodiazepine receptors: identification and characterization in central nervous system (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-06-11
    Description: Receptors that selectively bind micromolar concentrations of benzodiazepines are present in rat brain membrane. These micromolar receptors exhibit saturable, stereospecific binding, and the potency of benzodiazepine binding to these receptors is correlated with the ability of the benzodiazepines to inhibit maximum electric shock-induced convulsions. Benzodiazepine receptors with nanomolar affinity differ from the micromolar receptors in their binding, kinetic, and pharmacologic characteristics. The micromolar receptors also bind phenytoin, a non-benzodiazepine anticonvulsant. These results provide evidence for a distinct class of clinically relevant benzodiazepine receptors that may regulate neuronal excitability and anticonvulsant activity.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Bowling, A C -- DeLorenzo, R J -- NS 1352/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1982 Jun 11;216(4551):1247-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281893" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Benzodiazepines/*metabolism/pharmacology ; Benzodiazepinones/metabolism ; Brain/*metabolism ; Calmodulin/antagonists & inhibitors ; Diazepam/metabolism ; Kinetics ; Ligands ; Protein Kinase Inhibitors ; Rats ; Receptors, Drug/*metabolism ; Receptors, GABA-A ; Structure-Activity Relationship
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  • 16
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    Artificial enzymes (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-05
    Description: Simple chemical catalysts have been designed to achieve some desirable features of enzymes. These novel catalysts are not proteins, but they may incorporate the typical enzyme catalytic groups and they achieve selectivity in their reactions by use of geometric control, as do enzymes. Catalysts that carry out geometrically controlled chlorinations of aromatic rings and steroids have been constructed. Other catalysts achieve the selective synthesis of amino acids, and still others imitate ribonuclease in detailed mechanism and hydrolyze RNA. Optimization of geometries has led to a rate acceleration of over 10(8) in one instance.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Breslow, R -- New York, N.Y. -- Science. 1982 Nov 5;218(4572):532-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7123255" target="_blank"〉PubMed〈/a〉
    Keywords: Catalysis ; Cyclodextrins ; *Enzymes ; Kinetics ; Models, Chemical ; Ribonucleases ; Structure-Activity Relationship ; Substrate Specificity ; Transaminases
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  • 17
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    Stereoisomers of N-allylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-01-08
    Description: (+/-)-N-Allylnormetazocine is a benzomorphan opioid with psychotomimetic effects. The pure stereoisomers of this compound, as well as the racemic mixture, were compared to phencyclidine for their behavioral effects on squirrel monkeys and rats trained to discriminate phencyclidine from saline. Dose-response determinations were made for responses to phencyclidine, to a racemic mixture of N-allylnormetazocine, and to the pure levo and dextro isomers of N-allylnormetazocine. In both rats and monkeys, the dextro isomer and the racemic mixture produced dose-dependent responses appropriate for phencyclidine; the levo isomer did not produce the responses appropriate for phencyclidine at any of the doses tested. In both species, the levo isomer was more potent than the dextro isomer in decreasing the rate of responding. Thus racemic N-allylnormetazocine is a mixture of compounds that produce different behavioral effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Brady, K T -- Balster, R L -- May, E L -- DA-00490/DA/NIDA NIH HHS/ -- DA-01442/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1982 Jan 8;215(4529):178-80.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6274022" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Behavior, Animal/*drug effects ; Male ; Naloxone/pharmacology ; Phenazocine/*analogs & derivatives/pharmacology ; Phencyclidine/pharmacology ; Rats ; Rats, Inbred Strains ; Receptors, Opioid/drug effects ; Saimiri ; Stereoisomerism ; Structure-Activity Relationship
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  • 18
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    Alpha-substituted gamma-butyrolactones: new class of anticonvulsant drugs (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-09-10
    Description: Alkyl-Substituted gamma-butyrolactones were synthesized and tested for their convulsant and anticonvulsant actions in mice and guinea pigs. The alpha-substituted compounds, alpha, alpha-dimethyl-, and alpha-ethyl-alpha-methyl-gamma-butyrolactone were anticonvulsant compounds with a spectrum of activity similar to that of ethosuximide. In contrast, beta-substituted compounds were convulsant agents similar to picrotoxinin. The alpha-substituted-gama-butyrolactones represent a new class of anticonvulsant drug with experimental and clinical potential.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Klunk, W E -- McKeon, A -- Covey, D F -- Ferrendelli, J A -- GM-07200/GM/NIGMS NIH HHS/ -- GM-24483/GM/NIGMS NIH HHS/ -- NS-14834/NS/NINDS NIH HHS/ -- etc. -- New York, N.Y. -- Science. 1982 Sep 10;217(4564):1040-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6810462" target="_blank"〉PubMed〈/a〉
    Keywords: *4-Butyrolactone/analogs & derivatives/*therapeutic use/toxicity ; Animals ; *Anticonvulsants ; Chemical Phenomena ; Chemistry ; Convulsants ; Drug Evaluation, Preclinical ; Electroencephalography ; Epilepsy, Absence/drug therapy ; Ethosuximide/pharmacology ; *Furans/*therapeutic use ; Guinea Pigs ; Mice ; Structure-Activity Relationship ; Trimethadione/pharmacology
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 19
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    Purinergic regulation of food intake (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-07-02
    Description: Inosine peripherally administered to rats markedly suppressed spontaneous food intake and food intake induced by diazepam, muscimol, insulin, and food deprivation. The purines 2-deoxyguanosine and 2-deoxyinosine also suppressed food deprivation-induced feeding, whereas 7-methylinosine, which does not bind to the benzodiazepine binding site in vitro, had no effect on food intake when compared with controls. These results suggest that purines may represent endogenous substances that regulate food intake through interactions with the benzodiazepine receptor.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Levine, A S -- Morley, J E -- New York, N.Y. -- Science. 1982 Jul 2;217(4554):77-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7046046" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Appetite/*drug effects ; Deoxyguanosine/pharmacology ; Diazepam/pharmacology ; Eating/*drug effects ; Food Deprivation ; Inosine/analogs & derivatives/pharmacology ; Insulin/pharmacology ; Male ; Muscimol/pharmacology ; Purines/*pharmacology ; Rats ; Rats, Inbred Strains ; Structure-Activity Relationship
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 20
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    Spectral character of sunlight modulates photosynthesis of previtamin D3 and its photoisomers in human skin (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-05-28
    Description: The photosynthesis of previtamin D3 from 7-dehydrocholesterol in human skin was determined after exposure to narrow-band radiation or simulated solar radiation. The optimum wavelengths for the production of previtamin D3 were determined to be between 295 and 300 nanometers. When human skin was exposed to 295-nanometer radiation, up to 65 percent of the original 7-dehydrocholesterol content was converted to previtamin D3. In comparison, when adjacent skin was exposed to simulated solar radiation, the maximum formation of previtamin D3 was about 20 percent. Major differences in the formation of lumisterol3, and tachysterol3 from previtamin D3 were also observed. It is concluded that the spectral character of natural sunlight has a profound effect on the photochemistry of 7-dehydrocholesterol in human skin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉MacLaughlin, J A -- Anderson, R R -- Holick, M F -- AM 27334/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1982 May 28;216(4549):1001-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6281884" target="_blank"〉PubMed〈/a〉
    Keywords: Cholecalciferol/*biosynthesis/metabolism ; Dehydrocholesterols/radiation effects ; Ergosterol/metabolism ; Humans ; In Vitro Techniques ; Isomerism ; Photochemistry ; Skin/*metabolism ; Spectrum Analysis ; Structure-Activity Relationship ; Ultraviolet Rays
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  • 21
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    Oxytocin induces maternal behavior in virgin female rats (1982)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1982-05-07
    Description: Intracerebroventricular administration of oxytocin to virgin female rats that had been ovariectomized and primed with estrogen 48 hours previously induced a rapid onset of full maternal behavior. The maternal behavior persisted and its incidence was dose-related. Tocinoic acid, the ring structure of oxytocin, also rapidly induced the onset of persistent, full maternal behavior. Arginine vasopressin induced persistent maternal behavior, but this behavior had a later onset. Prostaglandin F2 alpha induced strong partial maternal behavior, which showed early onset but did not persist. Many other peptides, ovarian steroids, and prostaglandin E2 were no more effective than saline. These findings suggest that the release of oxytocin and prostaglandin F2 alpha during labor may promote maternal behavior in rats.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Pedersen, C A -- Ascher, J A -- Monroe, Y L -- Prange, A J Jr -- MH-22536/MH/NIMH NIH HHS/ -- MH-32316/MH/NIMH NIH HHS/ -- MH-34933/MH/NIMH NIH HHS/ -- New York, N.Y. -- Science. 1982 May 7;216(4546):648-50.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7071605" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arginine Vasopressin/pharmacology ; Brain/physiology ; Female ; Injections, Intraventricular ; *Maternal Behavior ; Oxytocin/administration & dosage/*pharmacology ; Rats ; Structure-Activity Relationship
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  • 22
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    Translational efficiency of transfer RNA's: uses of an extended anticodon (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-12
    Description: Transfer RNA's are probably very strongly selected for translational efficiency. In this article, the argument is presented that the coding performance of the triplet anticodon is enhanced by selection of a matching anticodon loop and stem sequence. the anticodon plus these nearby sequence features (the extended anticodon) therefore contains more coding information than the anticodon alone and can perform more efficiently and accurately at the ribosome. This idea successfully accounts for the relative efficiencies of many transfer RNA's.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Yarus, M -- New York, N.Y. -- Science. 1982 Nov 12;218(4573):646-52.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6753149" target="_blank"〉PubMed〈/a〉
    Keywords: Base Sequence ; Escherichia coli/genetics ; Kinetics ; Nucleic Acid Conformation ; *Protein Biosynthesis ; RNA, Transfer/*genetics ; Ribosomes/metabolism ; Structure-Activity Relationship ; Suppression, Genetic
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  • 23
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    Z-DNA moves toward "real biology" (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-11-04
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kolata, G -- New York, N.Y. -- Science. 1983 Nov 4;222(4623):495-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6623088" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Dna ; Eukaryota/genetics ; Humans ; *Nucleic Acid Conformation ; Species Specificity ; Structure-Activity Relationship
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 24
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    Antibodies that react with predetermined sites on proteins (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-02-11
    Description: Contrary to previous predictions, relatively short synthetic peptides that mimic part of a protein sequence are routinely capable of eliciting an antiserum that reacts with the partially mimicked protein. Peptides capable of eliciting protein-reactive serums are frequently represented in the primary sequence of a protein, can be characterized by a set of simple chemical rules, and are confined neither to immunodominant regions of intact proteins nor to the amino or carboxyl terminals. As such, synthetic peptide immunogens are valuable for eliciting reagents with predetermined specificity that can be used for basic research. In addition, some synthetic peptides are capable of mimicking regions of virus proteins and eliciting immune responses in animals that are protective against the viral agents. Such peptides may thus serve as the basis for safe, chemically defined synthetic vaccines.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Sutcliffe, J G -- Shinnick, T M -- Green, N -- Lerner, R A -- R01 AI 18509/AI/NIAID NIH HHS/ -- New York, N.Y. -- Science. 1983 Feb 11;219(4585):660-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6186024" target="_blank"〉PubMed〈/a〉
    Keywords: *Antibody Specificity ; Cross Reactions ; *Epitopes ; Peptides/immunology ; Proteins/*immunology ; Structure-Activity Relationship ; Vaccines/immunology
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  • 25
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    Monoclonal antibodies reveal the structural basis of antibody diversity (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-11-18
    Description: Hybridoma technology has made it possible to introduce into continuous culture normal antibody-forming cells and to obtain large amounts of the immunoglobulin produced by each of these cells. Examination of the structure of a number of monoclonal antibodies that react with a single antigen has provided new information on the structural basis of the specificity and affinity of antibodies. Comparisons of families of monoclonal antibodies derived from a single germ line gene revealed the importance of somatic mutation in generating antibody diversity. Monoclonal antibodies that react with variable regions of other monoclonals allow the further dissection and modulation of the immune response. Finally, the continued somatic instability of immunoglobulin genes in cultured antibody-forming cells makes it possible to determine the rate of somatic mutation and to generate mutant monoclonal antibodies that may be more effective serological reagents.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Teillaud, J L -- Desaymard, C -- Giusti, A M -- Haseltine, B -- Pollock, R R -- Yelton, D E -- Zack, D J -- Scharff, M D -- 5T32GM7288/GM/NIGMS NIH HHS/ -- AI05231/AI/NIAID NIH HHS/ -- AI10702/AI/NIAID NIH HHS/ -- New York, N.Y. -- Science. 1983 Nov 18;222(4625):721-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6356353" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Antibodies, Monoclonal/genetics/*immunology ; *Antibody Diversity ; Antibody Specificity ; Genes ; Hybridomas/immunology ; Immunoglobulin Idiotypes/immunology ; Immunoglobulin Variable Region/genetics ; Mice ; Mutation ; Protein Conformation ; Structure-Activity Relationship
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  • 26
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    Benzoquinolinediones: activity as insect teratogens (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-10-28
    Description: Morphological abnormalities including extra compound eyes, extra heads, and distally duplicated legs were generated in cricket embryos by treating eggs with single doses of either benz[g]isoquinoline-5,10-dione or benzo[h]quinoline-5,6-dione. Slight structural modifications of the molecules resulted in a loss of teratogenic activity, although embryotoxicity occurred. These potent insect teratogens can be used for analysis of developmental events during embryogenesis.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Walton, B T -- Ho, C -- Ma, C Y -- O'Neill, E G -- Kao, G L -- New York, N.Y. -- Science. 1983 Oct 28;222(4622):422-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6623081" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Isoquinolines/*toxicity ; Orthoptera/*embryology ; Quinolines/*toxicity ; *Quinolones ; Structure-Activity Relationship ; *Teratogens
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  • 27
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    Inhibition of dihydropteridine reductase by novel 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogs (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-04-27
    Description: Hydroxylated derivatives of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), a nigrostriatal neurotoxin in humans and primates, noncompetitively inhibited dihydropteridine reductase from human liver and rat striatal synaptosomes in vitro at micromolar concentrations. In contrast, MPTP and its chloro- and norderivatives did not inhibit this enzyme at lower than millimolar concentrations. Dihydropteridine reductase converts dihydrobiopterin to tetrahydrobiopterin, the required cofactor for the hydroxylation of aromatic amino acids during the synthesis of dopamine and serotonin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Abell, C W -- Shen, R S -- Gessner, W -- Brossi, A -- HD 14635/HD/NICHD NIH HHS/ -- New York, N.Y. -- Science. 1984 Apr 27;224(4647):405-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6608790" target="_blank"〉PubMed〈/a〉
    Keywords: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine ; Animals ; Corpus Striatum/enzymology ; Dihydropteridine Reductase/*antagonists & inhibitors ; Humans ; Hydroxylation ; Liver/enzymology ; NAD/metabolism ; NADH, NADPH Oxidoreductases/*antagonists & inhibitors ; Pyridines/*pharmacology ; Rats ; Structure-Activity Relationship ; Synaptosomes/enzymology
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 28
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    Nucleotide sequence of a human Blym transforming gene activated in a Burkitt's lymphoma (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-08-03
    Description: The nucleotide sequence of a human Blym-1 transforming gene activated in a Burkitt's lymphoma cell line was determined. This sequence predicts a small protein of 58 amino acids that is 33 percent identical to the predicted product of chicken Blym-1, the activated transforming gene of chicken B cell lymphomas. Both the human and chicken Blym-1 genes exhibit significant identity to an amino-terminal region of transferrins.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Diamond, A -- Devine, J M -- Cooper, G M -- CA 07250/CA/NCI NIH HHS/ -- CA 28946/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1984 Aug 3;225(4661):516-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6330897" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Base Sequence ; Burkitt Lymphoma/*genetics ; Cell Line ; *Cell Transformation, Neoplastic ; DNA Restriction Enzymes ; Humans ; *Oncogenes ; Structure-Activity Relationship ; Transcription, Genetic ; Transferrin/genetics
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  • 29
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    Activation of antitumor agent gilvocarcins by visible light (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-01-06
    Description: Gilvocarcins that are antitumor agents are activated by low doses of visible light to induce bacteriophage lambda in Escherichia coli. This result is dependent on interaction with DNA. Gilvocarcin M, an analog without antitumor activity, failed to induce the prophage after light exposure, thus demonstrating a correlation between photosensitizing and antitumor activities. These results raise several possibilities regarding the mode of action of gilvocarcins as antitumor agents in vivo, involving light or enzymatic activating systems, which could be exploited in human cancer therapy.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Elespuru, R K -- Gonda, S K -- New York, N.Y. -- Science. 1984 Jan 6;223(4631):69-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6229029" target="_blank"〉PubMed〈/a〉
    Keywords: *Aminoglycosides ; *Anti-Bacterial Agents ; Antibiotics, Antineoplastic/*pharmacology/radiation effects ; Bacteriophage lambda/growth & development ; Benzopyrans ; Coumarins ; Glycosides/pharmacology/radiation effects ; *Light ; Methoxsalen/pharmacology ; Structure-Activity Relationship ; Trioxsalen/pharmacology ; Ultraviolet Rays ; Virus Activation/*drug effects
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    Amphiphilic secondary structure: design of peptide hormones (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-01-20
    Description: Peptide synthesis can be used for elucidating the roles of secondary structures in the specificity of hormones, antigens, and toxins. Intermediate sized peptides with these activities assume amphiphilic secondary structures in the presence of membranes. When models are designed to optimize the amphiphilicity of the secondary structure, stronger interactions can be observed with the synthetic peptides than with the naturally occurring analogs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kaiser, E T -- Kezdy, F J -- HL-18577/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1984 Jan 20;223(4633):249-55.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6322295" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Apolipoprotein A-I ; Apolipoproteins ; Binding Sites ; Calcitonin ; Chemical Phenomena ; Chemistry ; Corticotropin-Releasing Hormone ; Endorphins ; Glucagon ; Growth Hormone-Releasing Hormone ; *Hormones/pharmacology ; Lipoproteins, HDL ; Melitten ; Models, Structural ; *Peptides/chemical synthesis/metabolism/pharmacology ; Protein Conformation ; Structure-Activity Relationship ; beta-Endorphin
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  • 31
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    A model study of fecapentaenes: mutagens of bacterial origin with alkylating properties (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-08-03
    Description: Fecapentaene-14 and -12 are directly acting mutagens that do not require metabolic activation. Their unusual structure suggests a possible mechanism of action. A carbocation that is formed by the addition of an electrophilic species (such as a proton) to the enol ether is most probably the reactive species. A series of model enol ethers with conjugated systems of various lengths was prepared, and a correlation between mutagenicity and increasing reactivity of derived carbocations was found. The glycerol moiety does not play a crucial role in the overall reactivity of the fecapentaenes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gupta, I -- Suzuki, K -- Bruce, R W -- Krepinsky, J J -- Yates, P -- New York, N.Y. -- Science. 1984 Aug 3;225(4661):521-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6377497" target="_blank"〉PubMed〈/a〉
    Keywords: *Alkylating Agents ; Mutagenicity Tests ; Mutagens/*toxicity ; *Mutation ; Polyenes/toxicity ; Salmonella typhimurium/drug effects ; Structure-Activity Relationship
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  • 32
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    Inhibitors of poly(adenosine diphosphate-ribose) synthesis: effect on other metabolic processes (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-02-10
    Description: 3-Aminobenzamide and benzamide, purported to be specific inhibitors of the synthesis of poly(adenosine diphosphate-ribose), were used to elucidate possible functions of this biopolymer. These compounds, at frequently used experimental concentrations, not only inhibited the action of poly(adenosine diphosphate-ribose) synthetase but also affected cell viability, glucose metabolism, and DNA synthesis. Thus, the usefulness of 3-aminobenzamide and benzamide may be severely restricted by the difficulty of finding a dose small enough to inhibit the synthetase without producing additional metabolic effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Milam, K M -- Cleaver, J E -- New York, N.Y. -- Science. 1984 Feb 10;223(4636):589-91.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6420886" target="_blank"〉PubMed〈/a〉
    Keywords: Benzamides/*toxicity ; Cell Line ; DNA Replication/drug effects ; Humans ; Kinetics ; Lymphocytes ; Nucleoside Diphosphate Sugars/*biosynthesis ; Poly Adenosine Diphosphate Ribose/*biosynthesis ; Poly(ADP-ribose) Polymerases/metabolism ; Structure-Activity Relationship
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  • 33
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    Carbocyclic arabinofuranosyladenine (cyclaradine): efficacy against genital herpes in guinea pigs (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-30
    Description: Carbocyclic arabinofuranosyladenine (cyclaradine), a novel nucleoside analog with such desired features as hydrolytic and enzymatic stability, adenosine deaminase resistance, and low systemic toxicity, inhibited the replication of herpes simplex virus types 1 and 2. The 5'-methoxyacetate prodrug form exhibited significant efficacy in the topical treatment of genital infections by herpes simplex virus type 2.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Vince, R -- Daluge, S -- Lee, H -- Shannon, W M -- Arnett, G -- Schafer, T W -- Nagabhushan, T L -- Reichert, P -- Tsai, H -- CA 23263/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Sep 30;221(4618):1405-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6684328" target="_blank"〉PubMed〈/a〉
    Keywords: Acyclovir/therapeutic use ; Animals ; Disease Models, Animal ; Female ; Guinea Pigs ; Herpes Genitalis/*drug therapy ; Male ; Structure-Activity Relationship ; Vidarabine/*analogs & derivatives/therapeutic use
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  • 34
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    Nicarbazin complex yields dinitrocarbanilide as ultrafine crystals with improved anticoccidial activity (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-11-11
    Description: Nicarbazin, a drug used to control the protozoal disease coccidiosis in poultry, is a complex of the highly insoluble drug 4,4'-dinitrocarbanilide with 2-hydroxy-4,6-dimethylpyrimidine. The structures of this and other 4,4'-dinitrocarbanilide complexes have not been determined, but an analogous 2:1 complex of 4,4'-dinitrodiphenylamine with 1,4-diacetylpiperazine has been prepared in which the only possible bonds are hydrogen bonds between the amide carbonyls and amino hydrogens. Scanning electron microscopy revealed that micron-size crystals of nicarbazin disintegrate in water to form much smaller dinitrocarbanilide crystals. Similar complex dissolution in the gut of poultry may account for the greater effectiveness of dinitrocarbanilide when administered as complexed rather than uncomplexed drug. Particle size problems associated with other highly insoluble drugs and pesticides may be resolved by the use of nicarbazin-like complexes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rogers, E F -- Brown, R D -- Brown, J E -- Kazazis, D M -- Leanza, W J -- Nichols, J R -- Ostlind, D A -- Rodino, T M -- New York, N.Y. -- Science. 1983 Nov 11;222(4624):630-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6635662" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Carbanilides/*administration & dosage ; Chickens ; Coccidiostats ; Crystallization ; Intestinal Absorption ; Nicarbazin/*administration & dosage ; Poultry Diseases/*prevention & control ; Solubility ; Structure-Activity Relationship
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    Bromine residue at hydrophilic region influences biological activity of aplysiatoxin, a tumor promoter (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-12-16
    Description: Aplysiatoxin and debromoaplysiatoxin, which are isolated from the seaweed, Lyngbya gracilis, differ in their chemical structure only by the presence or absence of a bromine residue in the hydrophilic region. The function and the structure-activity relation of the hydrophilic region are not known. Aplysiatoxin increased malignant transformation, stimulated DNA synthesis, and inhibited the binding of phorbol-12,13-dibutyrate and epidermal growth factor to cell receptors. Debromoaplysiatoxin inhibited the binding of these two substances as strongly as aplysiatoxin but did not increase malignant transformation or stimulate DNA synthesis. These results indicate that a slight change in the chemical structure of the hydrophilic region of aplysiatoxin affects its abilities to increase cell transformation and stimulate DNA synthesis and that the abilities of the tumor promoters to inhibit the binding of phorbol-12,13-dibutyrate and epidermal growth factor are dissociable from their abilities to increase cell transformation and stimulate DNA synthesis under some circumstances.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Shimomura, K -- Mullinix, M G -- Kakunaga, T -- Fujiki, H -- Sugimura, T -- New York, N.Y. -- Science. 1983 Dec 16;222(4629):1242-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6316505" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Caenorhabditis elegans Proteins ; Carcinogens/*pharmacology ; Carrier Proteins ; Cell Line ; Cell Transformation, Neoplastic/*drug effects ; Chemical Phenomena ; Chemistry ; DNA/biosynthesis ; Epidermal Growth Factor/metabolism ; Lactones/analysis/*pharmacology ; *Lyngbya Toxins ; Mice ; Phorbol 12,13-Dibutyrate ; Phorbol Esters/metabolism ; *Protein Kinase C ; Receptor, Epidermal Growth Factor ; Receptors, Cell Surface/metabolism ; *Receptors, Drug ; Structure-Activity Relationship
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    Rat transforming growth factor type 1: structure and relation to epidermal growth factor (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-03-09
    Description: The complete amino acid sequence of rat transforming growth factor type 1 has been determined. This growth factor, obtained from retrovirus-transformed fibroblasts, is structurally and functionally related to mouse epidermal growth factor and human urogastrone. Production of this polypeptide by various neoplastic cells might contribute to the continued expression of the transformed phenotype.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Marquardt, H -- Hunkapiller, M W -- Hood, L E -- Todaro, G J -- New York, N.Y. -- Science. 1984 Mar 9;223(4640):1079-82.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6320373" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Cell Line ; *Cell Transformation, Neoplastic ; DNA/biosynthesis ; Epidermal Growth Factor/*metabolism/pharmacology ; Humans ; Idoxuridine/metabolism ; Mice ; Peptide Biosynthesis ; Peptides/*metabolism/pharmacology ; Rats ; Receptor, Epidermal Growth Factor ; Receptors, Cell Surface/metabolism ; Structure-Activity Relationship ; Transforming Growth Factors
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    Need a catalyst? Design an enzyme (1984)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1984-01-20
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H 2nd -- New York, N.Y. -- Science. 1984 Jan 20;223(4633):269-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6608147" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Binding Sites ; Biochemistry/*methods ; Catalysis ; *Cloning, Molecular ; Enzymes/genetics/*metabolism ; Mutation ; Structure-Activity Relationship ; Substrate Specificity ; Tetrahydrofolate Dehydrogenase/metabolism ; Tyrosine-tRNA Ligase/metabolism ; beta-Lactamases/metabolism
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  • 38
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    Ala-Gly- and Val-Asp-[Arg8]-vasopressin: bovine storage forms of arginine vasopressin with natriuretic activity (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-02-22
    Description: Extracts of fresh-frozen bovine neurohypophysis were purified by chromatographic techniques to isolate and characterize the components that produce natriuresis in nondiuretic dogs. Two compounds with natiuretic properties similar to those of synthetic arginine vasopressin accounted for most of the natriuretic activity and appeared to be the prevalent vasopressin-like molecules in the extract. These peptides were Ala-Gly-[Arg8]-vasopressin and Val-Asp-[Arg8]-vasopressin; the natriuretic potency of each appeared to be similar to synthetic arginine vasopressin and could be observed with doses in the range of 50 picomoles. In the dog the most conspicuous difference between synthetic arginine vasopressin and the new vasopressin peptides was the smaller pressor responses to natriuretic doses of the new compounds.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gitelman, H J -- Klapper, D G -- Alderman, F R -- Blythe, W B -- New York, N.Y. -- Science. 1980 Feb 22;207(4433):893-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7355269" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Arginine Vasopressin/analogs & derivatives/*metabolism/pharmacology ; Biological Assay ; Blood Pressure/drug effects ; Cattle ; Dogs ; Male ; Natriuresis/*drug effects ; Pituitary Gland, Posterior/*metabolism ; Protein Precursors/metabolism ; Structure-Activity Relationship
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  • 39
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    Tumor-promoting phorbol esters stimulate hematopoietic colony formation in vitro (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-04-25
    Description: Tumor-promoting phorbol esters stimulated mouse bone marrow cells to form myeloid colonies in agar cultures without added colony-stimulating factors. The colony-stimulating ability of various phorbol esters correlated well with their ability to promote skin tumors in vivo. These results suggest that phorbol esters mimic the action of specific colony-stimulating factors that regulate growth.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Stuart, R K -- Hamilton, J A -- New York, N.Y. -- Science. 1980 Apr 25;208(4442):402-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6245446" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Division/drug effects ; Cells, Cultured ; *Colony-Forming Units Assay ; Colony-Stimulating Factors/pharmacology ; Dose-Response Relationship, Drug ; Hematopoietic Stem Cells/*drug effects ; Macrophages/physiology ; Mice ; Monocytes/physiology ; Phorbol Esters/pharmacology ; Phorbols/*pharmacology ; Receptors, Cell Surface/drug effects ; Structure-Activity Relationship ; Tetradecanoylphorbol Acetate/*pharmacology
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  • 40
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    Somatomedin B: mitogenic activity derived from contaminant epidermal growth factor (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-09-04
    Description: The mitogenic effect of somatomedin B on human cultured glial cells was neutralized by the addition of antibodies to mouse epidermal growth factor. Somatomedin B contained epidermal growth factor--like activity, competing for binding to the epidermal growth factor receptor. It is concluded that contaminating epidermal growth factor may explain the entire mitogenic activity of somatomedin B.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Heldin, C H -- Wasteson, A -- Fryklund, L -- Westermark, B -- New York, N.Y. -- Science. 1981 Sep 4;213(4512):1122-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6973821" target="_blank"〉PubMed〈/a〉
    Keywords: Cell Division/drug effects ; Cells, Cultured ; Epidermal Growth Factor/*pharmacology ; Growth Substances/*pharmacology ; Humans ; Neuroglia ; Peptides/*pharmacology ; Somatomedins/*pharmacology ; Structure-Activity Relationship
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    Peripherally administered reduced pterins do enter the brain (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-05-22
    Description: The content of tetrahydrobiopterin in rat brain was doubled by peripherally administered tetrahydrobiopterin, with the natural 1 diastereoisomer more effective than the unnatural d configuration. The model pteridine, 6-methyltetrahydropterin was ten times more efficient than tetrahydrobiopterin in crossing the blood-brain barrier, and striatal concentrations of 6-methyltetrahydropterin remained elevated for 2 hours, declining with a half-life of 3 hours. While no evidence for a specific uptake mechanism for concentrating 6-methyltetrahydropterin in cells containing tetrahydrobiopterin was detected, the pterin was found in ts presumed site of action, the nerve terminal. Replacement therapy with reduced pterins may therefore be effective in the treatment of the neurological disorders associated with the variant forms of hyperphenylalaninemia that result from defects in the biosynthesis or metabolism of tetrahydrobiopterin within the central nervous system.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Kapatos, G -- Kaufman, S -- New York, N.Y. -- Science. 1981 May 22;212(4497):955-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233193" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Biopterin/analogs & derivatives/*metabolism ; Blood-Brain Barrier ; Brain/*metabolism ; Male ; Pteridines/*metabolism ; Pterins/*metabolism ; Rats ; Stereoisomerism ; Structure-Activity Relationship
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    Odor quality: semantically generated multidimensional profiles are stable (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-11-19
    Description: Odors of ten compounds were characterized by approximately 150 subjects who used a list of 146 descriptors. Duplicate profiles correlated highly (P less than .001) and consistently higher than profiles of different odors. Profiles also agreed with those obtained previously. Thus, profiles based on combined responses of many subjects are stable constructs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Dravnieks, A -- New York, N.Y. -- Science. 1982 Nov 19;218(4574):799-801.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7134974" target="_blank"〉PubMed〈/a〉
    Keywords: *Alcohols ; Anisoles ; Hexanols ; Humans ; *Odors ; Pyridines ; *Smell ; Structure-Activity Relationship
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  • 43
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    Spinal sympathetic neurons: possible sites of opiate-withdrawal suppression by clonidine (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-03-26
    Description: Morphine, methadone, meperidine, fentanyl, and clonidine rapidly depressed transmission through sympathetic preganglionic neurons in cats with the spinal cord transected. Naloxone promptly antagonized this effect of the opiates but not that of clonidine which was reversed by alpha 2-adrenergic receptor antagonists. The independent depression of preganglionic neurons by clonidine may contribute to the ability of this drug to depress the symptoms of opiate withdrawal that are characterized by sympathetic hyperactivity.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Franz, D N -- Hare, D B -- McCloskey, K L -- GM-07579/GM/NIGMS NIH HHS/ -- HL-24085/HL/NHLBI NIH HHS/ -- RR-05428/RR/NCRR NIH HHS/ -- New York, N.Y. -- Science. 1982 Mar 26;215(4540):1643-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6280276" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cats ; Clonidine/*pharmacology/therapeutic use ; Evoked Potentials/drug effects ; Humans ; Narcotics/pharmacology ; Receptors, Drug/drug effects ; Reflex/drug effects ; Spinal Cord/cytology ; Structure-Activity Relationship ; Substance Withdrawal Syndrome/*drug therapy ; Sympathetic Nervous System/*drug effects ; Synaptic Transmission/*drug effects
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    DNA conformation, dynamics, and interactions in solution (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-05-07
    Description: The conformation and dynamics of the d(CGCGAATTCGCG) duplex, its analogs containing mismatched base pairs and helix interruptions, and its complexes with actinomycin and Netropsin, bound separately and simultaneously, have been investigated by nuclear magnetic resonance spectroscopy in aqueous solution. Structural information has been deduced from chemical shift and nuclear Overhauser effect parameters, while the kinetics have been probed from line width and saturation recovery experiments on proton and phosphorus markers at the individual base pair level. These studies lead to an improved understanding of the role of nucleic acid sequence on the structure, flexibility, and conformational interconversions in the duplex state. The nuclear magnetic resonance measurements readily identify helix modification and antibiotic binding sites on the nucleic acid and estimate the extent to which the observed conformational and dynamic perturbations are transmitted to adjacent base pair regions.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Patel, D J -- Pardi, A -- Itakura, K -- New York, N.Y. -- Science. 1982 May 7;216(4546):581-90.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6280281" target="_blank"〉PubMed〈/a〉
    Keywords: Base Sequence ; Dna ; Dactinomycin ; Hydrogen Bonding ; Magnetic Resonance Spectroscopy ; Motion ; Netropsin ; *Nucleic Acid Conformation ; Oligodeoxyribonucleotides ; Protons ; Structure-Activity Relationship ; Temperature
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  • 45
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    (+)-Amphetamine binding to rat hypothalamus: relation to anorexic potency for phenylethylamines (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-10-29
    Description: Saturable and stereospecific binding sites for (+)-[3H]amphetamine were demonstrated in membrane preparations from rat brain. The density of these binding sites varies among brain regions and is highest in the hypothalamus and brainstem. Specific (+)-[3H]amphetamine binding in hypothalamus is largely confined to synaptosomal membranes, rapidly reversible, and sensitive to both heat and proteolytic enzymes. Scatchard analysis of the equilibrium binding data revealed two distinct sites with apparent affinity constants of 93 and 300 nanomoles per liter, respectively. The effects of various psychotropic drugs as well as a number of putative neurotransmitters and related agonists and antagonists in displacing specific (+)-[3H]amphetamine binding demonstrate that these binding sites are not associated with any previously described neurotransmitter or drug receptors, but are specific for amphetamine and related phenylethylamine derivatives. Furthermore, the relative affinities of a series of phenylethylamine derivatives for (+)-[3H]amphetamine binding sites in hypothalamic membranes is highly correlated to their potencies as anorexic agents. These results suggest the presence of specific receptor sites in hypothalamus that mediate the anorexic activity of amphetamine and related drugs.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Paul, S M -- Hulihan-Giblin, B -- Skolnick, P -- New York, N.Y. -- Science. 1982 Oct 29;218(4571):487-90.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7123250" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Anorexia/physiopathology ; Appetite Depressants/*pharmacology ; Cell Membrane/metabolism ; Dextroamphetamine/*metabolism ; Hypothalamus/drug effects/*metabolism/physiology ; Male ; Phenethylamines/metabolism ; Rats ; Receptors, Drug/*metabolism ; Structure-Activity Relationship
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  • 46
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    Nonopiate effects of dynorphin and des-Tyr-dynorphin (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-12-10
    Description: Intracerebroventricular administration of dynorphin produced potent and long-lasting effects on motor function and the electroencephalogram in rats. In addition, local iontophoretic or pressure ejection of dynorphin consistently inhibited hippocampal unit activity. None of these effects were significantly affected by naloxone even at high doses. Moreover, a fragment of dynorphin that failed to displace any of a number of tritiated narcotics from rat brain homogenates produced similar effects on these physiological measures in vivo. On the basis of a variety of criteria for "opiate action," the results suggest that a second biologically active site within the dynorphin sequence is capable of quite potent but nonopiate effects.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Walker, J M -- Moises, H C -- Coy, D H -- Baldrighi, G -- Akil, H -- 1F32DA04183/DA/NIDA NIH HHS/ -- DA02265/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1982 Dec 10;218(4577):1136-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6128791" target="_blank"〉PubMed〈/a〉
    Keywords: Action Potentials ; Amino Acid Sequence ; Animals ; Dynorphins ; Endorphins/*physiology ; Hippocampus/*physiology ; Male ; Pain/*physiopathology ; Rats ; Structure-Activity Relationship
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  • 47
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    A major metabolite of arginine vasopressin in the brain is a highly potent neuropeptide (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-09-23
    Description: A peptide that accumulated as the major product during the proteolysis of arginine vasopressin by rat brain synaptic membranes was isolated and its structure was shown to be the hexapeptide pGlu-Asn-Cys(Cys)-Pro-Arg-Gly-NH2. When administered intracerebroventricularly in extremely low doses, this vasopressin fragment and its desglycinamide derivative facilitated memory consolidation in a passive avoidance situation. These vasopressin metabolites, which are devoid of pressor activity, constitute highly potent neuropeptides with selective effects on memory and related processes; they are activated via proteolytic processing of vasopressin by brain peptidases.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Burbach, J P -- Kovacs, G L -- de Wied, D -- van Nispen, J W -- Greven, H M -- New York, N.Y. -- Science. 1983 Sep 23;221(4617):1310-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6351252" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Arginine Vasopressin/*metabolism/physiology ; Avoidance Learning/physiology ; Brain/*metabolism ; Dose-Response Relationship, Drug ; Male ; Memory/*physiology ; Oligopeptides/metabolism ; Peptide Hydrolases/metabolism ; Rats ; Structure-Activity Relationship
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    Heart imaging with cationic complexes of technetium (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-10-02
    Description: The cationic technetium-99 complex trans-[99TC(dmpe)2Cl2]+, where dmpe is bis(1,2-dimethylphosphino)ethane or (CH3)2P-CH2-P(CH3)2, has been prepared and characterized by single-crystal, x-ray structural analysis. The technetium-99m analog, trans-(99mTc(dmpe) 2Cl2]+, has also been prepared and shown to yield excellent gamma-ray images of the heart. The purposeful design, characterization, and synthesis of this technetium-99m radiopharmaceutical represents a striking application of fundamental inorganic chemistry to a problem in applied nuclear medicine.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Deutsch, E -- Bushong, W -- Glavan, K A -- Elder, R C -- Sodd, V J -- Scholz, K L -- Fortman, D L -- Lukes, S J -- HL-21276/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1981 Oct 2;214(4516):85-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6897930" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cations, Monovalent ; Dogs ; Heart/*radionuclide imaging ; *Organotechnetium Compounds ; *Phosphines ; Structure-Activity Relationship ; *Technetium
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  • 49
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    Elastin fragments attract macrophage precursors to diseased sites in pulmonary emphysema (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-05-22
    Description: This study suggests one mechanism by which alveolar macrophages accumulate in the lung in pulmonary emphysema: elastin fragments generated at the diseased sites are potent chemoattractants for monocytes, the precursors of the macrophages. The most chemotactic elastin fragments have a molecular weight between 10,000 and 50,000 and are active at concentrations as low as 3 nanograms per milliliter. By comparison, elastin fragments with higher molecular weights and desmosines are active at concentrations greater than 0.3 microgram per milliliter. In addition, preincubation of monocytes with the 10,000- to 50,000-dalton elastin impairs the ability of the cells to migrate toward elastin fragments but not toward activated serum. Fragments of tropoelastin are not chemotactic for monocytes. Because elastin, but not tropoelastin, contains lysyl-derived cross-links, these structures may be the active chemotactic site on the elastin fragments.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hunninghake, G W -- Davidson, J M -- Rennard, S -- Szapiel, S -- Gadek, J E -- Crystal, R G -- New York, N.Y. -- Science. 1981 May 22;212(4497):925-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7233186" target="_blank"〉PubMed〈/a〉
    Keywords: Cells, Cultured ; Chemotaxis, Leukocyte/*drug effects ; Dose-Response Relationship, Drug ; Elastin/*analogs & derivatives/*pharmacology ; Humans ; Macrophages/physiology ; Monocytes/*physiology ; Peptide Fragments/pharmacology ; Pulmonary Emphysema/*physiopathology ; Structure-Activity Relationship ; Tropoelastin/*pharmacology
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    A new generation of antibiotics (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-11
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Maugh, T H 2nd -- New York, N.Y. -- Science. 1981 Sep 11;213(4513):1238.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7268430" target="_blank"〉PubMed〈/a〉
    Keywords: Anti-Bacterial Agents/*isolation & purification ; Lactams/*isolation & purification ; Structure-Activity Relationship
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    Pineal N-acetyltransferase is inactivated by disulfide-containing peptides: insulin is the most potent (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-07-31
    Description: Pineal N-acetyltransferase can be inactivated in broken cell preparations by cystamine through a mechanism of thiol-disulfide exchange. Some, but not all, disulfide-containing peptides can inactivate this enzyme; the most potent inactivator is insulin. These findings suggest that a disulfide-containing peptide with high reactivity toward N-acetyltransferase may participate in the intracellular regulation of this enzyme.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Namboodiri, M A -- Favilla, J T -- Klein, D C -- New York, N.Y. -- Science. 1981 Jul 31;213(4507):571-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7017937" target="_blank"〉PubMed〈/a〉
    Keywords: Acetyltransferases/*antagonists & inhibitors ; Animals ; Disulfides/pharmacology ; Dithiothreitol/pharmacology ; Hormones/pharmacology ; Hydrogen-Ion Concentration ; Insulin/*pharmacology ; Kinetics ; Male ; Peptides/*pharmacology ; Pineal Gland/*enzymology ; Rats ; Structure-Activity Relationship
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    Cerebroventricular propranolol elevates cerebrospinal fluid norepinephrine and lowers blood pressure (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-08-21
    Description: Ventriculocisternal administration of dl- and d-propranolol produced dose-dependent increases in cerebrospinal fluid norepinephrine and reductions in blood pressure. A highly significant correlation was found between the increase in norepinephrine and the hypotensive effect. The propranolol-induced hypotension was prevented by intracisternal phentolamine. These data indicate that the hypotensive effect of centrally administered propranolol results from a drug-induced release of norepinephrine, which stimulates central alpha receptors to lower arterial pressure.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Tackett, R L -- Webb, J G -- Privitera, P J -- 5T32 HL07260-02/HL/NHLBI NIH HHS/ -- GM 20387/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1981 Aug 21;213(4510):911-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7256285" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Blood Pressure/*drug effects ; Dogs ; Injections, Intraventricular ; Isomerism ; Norepinephrine/*cerebrospinal fluid ; Propranolol/administration & dosage/*pharmacology ; Structure-Activity Relationship
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    Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin (1981)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1981-09-18
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Vale, W -- Spiess, J -- Rivier, C -- Rivier, J -- AM 18811/AM/NIADDK NIH HHS/ -- AM 20917/AM/NIADDK NIH HHS/ -- AM 26741/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 18;213(4514):1394-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6267699" target="_blank"〉PubMed〈/a〉
    Keywords: Adrenocorticotropic Hormone/*secretion ; Amino Acid Sequence ; Amphibian Proteins ; Angiotensinogen ; Animals ; Corticotropin-Releasing Hormone/*isolation & purification ; Endorphins/*secretion ; Hypothalamo-Hypophyseal System/physiology ; Peptide Hormones ; Peptides ; Pituitary Gland, Anterior/*secretion ; Pituitary Hormone-Releasing Hormones/*isolation & purification ; Radioimmunoassay ; Sheep ; Structure-Activity Relationship
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    Hyperglycemia of diabetic rats decreased by a glucagon receptor antagonist (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-02-26
    Description: The glucagon analog [l-N alpha-trinitrophenylhistidine, 12-homoarginine]-glucagon (THG) was examined for its ability to lower blood glucose concentrations in rats made diabetic with streptozotocin. In vitro, THG is a potent antagonist of glucagon activation of the hepatic adenylate cyclase assay system. Intravenous bolus injections of THG caused rapid decreases (20 to 35 percent) of short duration in blood glucose. Continuous infusion of low concentrations of the inhibitor led to larger sustained decreases in blood glucose (30 to 65 percent). These studies demonstrate that a glucagon receptor antagonist can substantially reduce blood glucose levels in diabetic animals without addition of exogenous insulin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Johnson, D G -- Goebel, C U -- Hruby, V J -- Bregman, M D -- Trivedi, D -- AM21085/AM/NIADDK NIH HHS/ -- AM25318/AM/NIADDK NIH HHS/ -- New York, N.Y. -- Science. 1982 Feb 26;215(4536):1115-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6278587" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Diabetes Mellitus, Experimental/*drug therapy ; Glucagon/*analogs & derivatives/*antagonists & inhibitors/therapeutic use ; Hyperglycemia/*drug therapy ; Male ; Rats ; Receptors, Cell Surface/*drug effects ; Receptors, Glucagon ; Structure-Activity Relationship
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    N-acetylation regulates the behavioral activity of alpha-melanotropin in a multineurotransmitter neuron (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-02-26
    Description: A multineurotransmitter neuronal system that synthesizes and secretes both acetylated and deacetylated forms of alpha-melantropin and beta-endorphin is present in rat and human brain. The N-acetylated from of alpha-melanotropin had more potent behavioral effects than the deacetylated alpha-melanotropin. In the case of beta-endorphin, however, the deacetylated form has been shown to be more potent than the acetylated form. Enzymatic N-acetylation appears to be an important regulatory process for modulating the behavioral activity of peptides secreted from the opiomelanotropinergic multineurotransmitter neuron.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉O'Donohye, T L -- Handelmann, G E -- Miller, R L -- Jacobowitz, D M -- New York, N.Y. -- Science. 1982 Feb 26;215(4536):1125-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7063845" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylation ; Animals ; Behavior, Animal/drug effects ; Brain/*metabolism ; Humans ; Melanocyte-Stimulating Hormones/*metabolism/pharmacology ; Neurons/metabolism ; Rats ; Structure-Activity Relationship
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    A 7-hydroxymethyl sulfate ester as an active metabolite of 7,12-dimethylbenz[alpha]anthracene (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-01-22
    Description: 7-Hydroxymethyl-12-methylbenz[alpha]anthracene (7-HMBA), a carcinogenic major metabolite of 7,12-dimethylbenz[alpha]anthracene (DMBA) in liver, was transformed by liver cytosolic sulfotransferase to reactive 7-HMBA sulfate, which is mutagenic toward Salmonella typhimurium strain TA98. The mutagenicity of 7-HMBA in the presence of hepatic sulfotransferase was much higher than that of DMBA or 7-HMBA in the presence of hepatic monooxygenase.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Watabe, T -- Ishizuka, T -- Isobe, M -- Ozawa, N -- New York, N.Y. -- Science. 1982 Jan 22;215(4531):403-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6800033" target="_blank"〉PubMed〈/a〉
    Keywords: 9,10-Dimethyl-1,2-benzanthracene/analogs & derivatives/*metabolism/pharmacology ; Benz(a)Anthracenes/*metabolism ; Biotransformation ; Mutagenicity Tests ; *Mutagens ; Salmonella typhimurium/drug effects ; Structure-Activity Relationship ; Sulfuric Acids
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    Ivermectin: a potent new antiparasitic agent (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-08-26
    Description: Ivermectin is the 22,23-dihydro derivative of avermectin B1, a macrocyclic lactone produced by an actinomycete, Streptomyces avermitilis. It is active at extremely low dosage against a wide variety of nematode and arthropod parasites, apparently by virtue of its action on the mediation of neurotransmission by gamma-aminobutyric acid. It is now in commercial use in various countries for the treatment and control of parasites in cattle, horses, and sheep, and is expected to become available for use in swine and dogs. Since studies with the drug in man are in a preliminary stage, it is not yet known whether ivermectin will be useful in human medicine.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Campbell, W C -- Fisher, M H -- Stapley, E O -- Albers-Schonberg, G -- Jacob, T A -- New York, N.Y. -- Science. 1983 Aug 26;221(4613):823-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6308762" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Anthelmintics ; Arthropods/drug effects ; Humans ; Insecticides/therapeutic use ; Ivermectin ; Lactones/metabolism/pharmacology/*therapeutic use ; Nematode Infections/*drug therapy ; Streptomyces/physiology ; Structure-Activity Relationship ; Synaptic Transmission/drug effects
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    Stereospecific action of pyrethroid insecticides on the gamma-aminobutyric acid receptor-ionophore complex (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-09-30
    Description: The potent alpha-cyano-3-phenoxybenzyl pyrethroids, including cypermethrin, deltamethrin, and fenvalerate, act stereospecifically to inhibit binding to rat brain synaptic membranes of sulfur-35-labeled t-butylbicyclophosphorothionate, a new radioligand for the picrotoxinin binding site. Scatchard analysis indicates that picrotoxinin inhibition of t-butylbicyclophosphorothionate binding is competitive whereas cypermethrin inhibition possibly involves a closely associated site in the gamma-aminobutyric acid receptor-ionophore complex. Studies with 37 pyrethroids reveal an absolute correlation, that is, no false positives or negatives, between mouse intracerebral toxicity and in vitro inhibition: all toxic cyano compounds but none of their nontoxic stereoisomers are inhibitors; cis isomers are more potent than trans isomers as both toxicants and inhibitors; and noncyano pyrethroids are much less potent or are inactive.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Lawrence, L J -- Casida, J E -- P01 ES00049/ES/NIEHS NIH HHS/ -- New York, N.Y. -- Science. 1983 Sep 30;221(4618):1399-401.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6310756" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bicyclo Compounds/metabolism ; *Bicyclo Compounds, Heterocyclic ; Binding, Competitive ; Brain/metabolism ; Insecticides/*pharmacology ; Ionophores/antagonists & inhibitors ; Picrotoxin/metabolism ; Protein Binding ; Pyrethrins/metabolism/*pharmacology ; Rats ; Receptors, Cell Surface/*drug effects/metabolism ; Receptors, GABA-A ; Stereoisomerism ; Structure-Activity Relationship ; Synaptic Membranes/metabolism
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    Spermidine requirement for cell proliferation in eukaryotic cells: structural specificity and quantitation (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-03-04
    Description: Six structural homologs of spermidine and five of its precursor, putrescine, were studied for their ability to prevent cytostasis of cultured L1210 leukemia cells induced by alpha-difluoromethylornithine (DFMO), a specific inhibitor of putrescine biosynthesis. High-performance liquid chromatography and competition studies with spermidine indicated that the homologs, which vary in the length of the carbon chain separating the amines, penetrated the cells. The structural specificity of the spermidine carrier was defined. Three of the six spermidine homologs supported cell growth during a 48-hour incubation in the presence of DFMO, indicating that a two-carbon extension of spermidine structure was tolerated for biological function. Two of the five putrescine homologs supported growth after being converted by the cells to their respective spermidine homologs. The central nitrogen of spermidine appears to be essential for function since diamines of chain length comparable to that of spermidine did not prevent DFMO cytostasis. No more than 15 percent of the spermidine normally present in L1210 cells was required for cell proliferation in the presence of DFMO.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Porter, C W -- Bergeron, R J -- CA-22153/CA/NCI NIH HHS/ -- CA-24538/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Mar 4;219(4588):1083-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6823570" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Cell Division ; *Cell Physiological Phenomena ; Eukaryotic Cells/*physiology ; Leukemia L1210/pathology ; Mice ; Ornithine Decarboxylase Inhibitors ; Putrescine/physiology ; Spermidine/analogs & derivatives/*physiology ; Structure-Activity Relationship
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    Bodian's silver method stains neurofilament polypeptides (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-09-25
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Gambetti, P -- Autilio Gambetti, L -- Papasozomenos, S C -- AG 00795/AG/NIA NIH HHS/ -- NS 14509/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1981 Sep 25;213(4515):1521-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6169146" target="_blank"〉PubMed〈/a〉
    Keywords: Cytoskeleton/*ultrastructure ; Electrophoresis, Polyacrylamide Gel ; Molecular Weight ; Proteins ; Silver ; *Staining and Labeling ; Structure-Activity Relationship
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    Metkephamid, a systemically active analog of methionine enkephalin with potent opioid alpha-receptor activity (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-02-06
    Description: Metkephamid is an analog of methionine enkephalin that retains high affinity for the delta receptor and is a systemically active analgesic. Since it is at least 100 times more potent than morphine as an analgesic when placed directly into the lateral ventricles, and is 30 to 100 times more potent on the delta receptor and yet is roughly equipotent on the mu receptor in vitro, it is concluded that it probably produces analgesia by action on delta receptors as well as, or rather than, on mu receptors. It has less tendency to produce respiratory depression, tolerance, and physical dependence than standard analgesics, and it is presently undergoing clinical trial.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Frederickson, R C -- Smithwick, E L -- Shuman, R -- Bemis, K G -- New York, N.Y. -- Science. 1981 Feb 6;211(4482):603-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6256856" target="_blank"〉PubMed〈/a〉
    Keywords: *Analgesics ; Animals ; Brain/*drug effects ; Dose-Response Relationship, Drug ; Endorphins/*pharmacology ; *Enkephalin, Methionine/*analogs & derivatives ; Enkephalins/*pharmacology ; Humans ; Kinetics ; Male ; Mice ; Rats ; Receptors, Opioid/*drug effects ; Structure-Activity Relationship ; Substance-Related Disorders/etiology
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    A substance P antagonist, [D-Pro2, D-Trp7,9]SP, inhibits inflammatory responses in the rabbit eye (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-11-27
    Description: Neurogenic factors released by antidromic nerve stimulation are thought to be in part responsible for the vasodilation and breakdown of the blood-aqueous barrier that follows trauma to the eye. Substance P is one candidate for the mediation of the inflammatory response since it is thought to be a neurotransmitter in sensory afferents and since exogenous substance P is capable of eliciting a response characteristic of inflammation. In rabbits, intravitreal or topical application onto the eye of a specific substance P antagonist, [d-Pro2, D-Trp7,9]SP, inhibited not only the irritant effects of exogenous substance P but also the inflammatory response to a standardized trauma (infrared irradiation of the iris). These observations suggest that substance P, or a related peptide, is a neurogenic mediator of the inflammatory response in the eye.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Holmdahl, G -- Hakanson, R -- Leander, S -- Rosell, S -- Folkers, K -- Sundler, F -- New York, N.Y. -- Science. 1981 Nov 27;214(4524):1029-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6171036" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Eye Diseases/*drug therapy ; Inflammation/*drug therapy ; Infrared Rays ; Pupil/drug effects/radiation effects ; Rabbits ; Structure-Activity Relationship ; Substance P/*analogs & derivatives/*antagonists & inhibitors/therapeutic use
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    Two distinct central serotonin receptors with different physiological functions (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-05-15
    Description: Two distinct serotonin (5-hydroxytryptamine) receptors designated serotonin 1 and serotonin 2 bind tritium-labeled serotonin and tritium-labeled spiroperidol, respectively. Drug potencies at serotonin 2 sites, but not at serotonin 1 sites, predict their effects on the "serotonin behavioral syndrome," indicating that serotonin 2 sites mediate these behaviors. The limited correlation of drug effects with regulation by guanine nucleotides suggests that serotonin 1 sites might be linked to adenylate cyclase. Drug specificities of serotonin-elicited synaptic inhibition and excitation may reflect serotonin 1 and serotonin 2 receptor interactions, respectively.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Peroutka, S J -- Lebovitz, R M -- Snyder, S H -- DA-00074/DA/NIDA NIH HHS/ -- New York, N.Y. -- Science. 1981 May 15;212(4496):827-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7221567" target="_blank"〉PubMed〈/a〉
    Keywords: Adenylyl Cyclases/metabolism ; Animals ; Behavior, Animal/*physiology ; Brain/*physiology ; Guanine Nucleotides/physiology ; Kinetics ; Male ; Rats ; Receptors, Serotonin/*physiology ; Serotonin/metabolism ; Spiperone/metabolism ; Structure-Activity Relationship
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    Vasopressin analogs that antagonize antidiuretic responses by rats to the antidiuretic hormone (1981)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1981-04-03
    Description: Four new synthetic analogs of vasopressin (antidiuretic hormone) can antagonize the antidiuretic response to intravenous vasopressin in anesthetized, water-loaded rats. They also cause a diuresis resembling that of diabetes insipidus when given intraperitoneally to conscious rats. Such antagonists may prove to be useful both pharmacologically and therapeutically.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Sawyer, W H -- Pang, P K -- Seto, J -- McEnroe, M -- Lammek, B -- Manning, M -- AM 01940/AM/NIADDK NIH HHS/ -- GM 25280/GM/NIGMS NIH HHS/ -- HL 12738/HL/NHLBI NIH HHS/ -- New York, N.Y. -- Science. 1981 Apr 3;212(4490):49-51.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7209515" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arginine Vasopressin/*analogs & derivatives/chemical synthesis/pharmacology ; Diuresis/*drug effects ; Female ; Osmolar Concentration ; Rats ; Structure-Activity Relationship ; Vasopressins/*antagonists & inhibitors
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    beta, gamma-Peroxy analogs of adenosine and guanosine triphosphate: synthesis and biological activity (1982)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1982-01-01
    Description: Extended analogs of adenosine triphosphate (ATP) and guanosine triphosphate (GTP), in which a peroxide bridge replaces the terminal bridge-oxygen of the triphosphate chain, have been synthesized. The ability of beta, gamma-peroxy-ATP to inhibit or substitute for ATP in representative enzyme systems and that of beta, gamma-peroxy-GTP, for FTP in protein synthesis was tested.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rosendahl, M S -- Leonard, N J -- GM-05829/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1982 Jan 1;215(4528):81-2.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7053563" target="_blank"〉PubMed〈/a〉
    Keywords: Adenosine Triphosphate/*analogs & derivatives/chemical synthesis/metabolism ; Guanosine Triphosphate/*analogs & derivatives/chemical synthesis/metabolism ; Kinetics ; Peroxides ; Protein Biosynthesis/drug effects ; Structure-Activity Relationship
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    Angiogenesis inhibition and tumor regression caused by heparin or a heparin fragment in the presence of cortisone (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-08-19
    Description: Heparin or a heparin fragment administered with cortisone inhibited angiogenesis, caused regression of large tumor masses, and prevented metastases. Oral administration of heparin resulted in the release of non-anticoagulant heparin fragments in the serum which, in the presence of cortisone, had similar anti-angiogenic and antitumor effects. Of all the heparin fragments tested, the most potent inhibition of angiogenesis in the presence of cortisone was provided by a hexasaccharide with a molecular weight of about 1600.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Folkman, J -- Langer, R -- Linhardt, R J -- Haudenschild, C -- Taylor, S -- EY04002/EY/NEI NIH HHS/ -- GM25810/GM/NIGMS NIH HHS/ -- R01-CA14019/CA/NCI NIH HHS/ -- New York, N.Y. -- Science. 1983 Aug 19;221(4612):719-25.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6192498" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Antineoplastic Agents ; Chick Embryo ; Cortisone/*pharmacology ; Heparin/*pharmacology ; Inflammation ; Neoplasm Metastasis ; Neoplasms, Experimental/blood supply ; Neovascularization, Pathologic/*physiopathology ; Oligosaccharides/pharmacology ; Rabbits ; Structure-Activity Relationship
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    Methadone conformation and opioid activity (1983)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1983-04-22
    Description: The inactive methadone analog threo-5-methylmethadone has a solid-state conformation in which the nitrogen is antiperiplanar to the tertiary carbon C(4). Since threo-5-methylmethadone exhibits no opioid agonism either in vivo or in vitro, methadone analogs probably do not have this conformation when bound to an opioid receptor. The potent agonist (-)-erythro-5-methylmethadone has a solid-state conformation in which the nitrogen atom is rotated back toward the phenyl rings on the quarternary carbon, suggesting that this unusual conformation is the active one.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Duax, W L -- Smith, G D -- Griffin, J F -- Portoghese, P S -- RR-05716/RR/NCRR NIH HHS/ -- New York, N.Y. -- Science. 1983 Apr 22;220(4595):417-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6301007" target="_blank"〉PubMed〈/a〉
    Keywords: Methadone/analogs & derivatives/*pharmacology ; Molecular Conformation ; Receptors, Opioid/metabolism ; Stereoisomerism ; Structure-Activity Relationship
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    Asymmetry of the acetylcholine channel revealed by quaternary anesthetics (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-10-10
    Description: Tissue-cultured rat myoballs were examined electrophysiologically with a suction pipette, which was used for voltage clamping and internal perfusion. The lidocaine derivative QX-314 caused a time- and membrane potentia-dependent block of acetylcholine-induced current only when applied from the extracellular membrane surface. The same compounds caused a use-dependent block of the sodium channel only from the intracellular membrane surface. These experiments demonstrate a fundamental asymmetry of the acetylcholine receptor-channel complex.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Horn, R -- Brodwick, M S -- Dickey, W D -- CA-19017/CA/NCI NIH HHS/ -- NS-12961/NS/NINDS NIH HHS/ -- NS-13778/NS/NINDS NIH HHS/ -- New York, N.Y. -- Science. 1980 Oct 10;210(4466):205-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6251552" target="_blank"〉PubMed〈/a〉
    Keywords: Acetylcholine/*metabolism ; Animals ; *Ion Channels/drug effects ; Lidocaine/*analogs & derivatives/pharmacology ; Membrane Potentials/drug effects ; Membrane Proteins ; Motor Endplate/*ultrastructure ; Neuromuscular Junction/*ultrastructure ; Rats ; *Receptors, Cholinergic ; Sodium/metabolism ; Structure-Activity Relationship
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    Angiotoxicity of oxygenated sterols and possible precursors (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-02-08
    Description: Cell death, inflammation, and repair in rabbits' aortas and pulmonary arteries were observed at 3-, 7-, and 10-day periods after the intravenous injection of oxygenated sterols. Thus, oxygenated sterols, not cholesterol, may play the primary role in arterial wall injury and lesion development.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Imai, H -- Werthessen, N T -- Subramanyam, V -- LeQuesne, P W -- Soloway, A H -- Kanisawa, M -- New York, N.Y. -- Science. 1980 Feb 8;207(4431):651-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7352277" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Aorta/drug effects ; Blood Vessels/*drug effects/pathology ; Cholesterol/*analogs & derivatives/toxicity ; Epoxy Compounds/*toxicity ; Ethers, Cyclic/*toxicity ; Female ; Hydroxycholesterols/toxicity ; Lanosterol/analogs & derivatives/toxicity ; Male ; Necrosis ; Oxidation-Reduction ; Pulmonary Artery/drug effects ; Rabbits ; Structure-Activity Relationship
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    Effect of interferon-alpha 1 from E. coli on some cell functions (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-09-19
    Description: Interferon-alpha 1 from Escherichia coli transformed with a hybrid plasmid containing a human leukocyte complementary DNA insert, induces resistance to virus in appropriate target cells. It also shares the following properties with natural leukocyte interferon (IFN). (i) It enhances natural killing activity of human lymphocytes, (ii) it enhances antibody-dependent cell-mediated cytotoxicity, (iii) it suppresses antigen- and mitogen-induced leukocyte migration inhibition, (iv) it inhibits growth of IFN-sensitive Burkitt lymphoma cells. Since these activities are exhibited by a cloned protein species, they are due to IFN itself and not to other human proteins.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Masucci, M G -- Szigeti, R -- Klein, E -- Klein, G -- Gruest, J -- Montagnier, L -- Taira, H -- Hall, A -- Nagata, S -- Weissmann, C -- New York, N.Y. -- Science. 1980 Sep 19;209(4463):1431-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6158096" target="_blank"〉PubMed〈/a〉
    Keywords: Antibody-Dependent Cell Cytotoxicity/drug effects ; Cell Division/drug effects ; Cell Migration Inhibition ; Cloning, Molecular ; *DNA, Recombinant ; Escherichia coli ; Humans ; Hypersensitivity, Delayed/immunology ; Immunity, Cellular/drug effects ; Interferons/genetics/*pharmacology ; Structure-Activity Relationship
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    At least three human type alpha interferons: structure of alpha 2 (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-09-19
    Description: The sequence of a human leukocyte-derived complementary DNA (cDNA), Hif-2h, which directs the formation in Escherichia coli of a polypeptide, IFN-alpha 1, with interferon (IFN) activity has been described. A second IFN cDNA, Hif-SN206, which also elicits synthesis of a biologically active IFN, IFN-alpha 2, is described in this article. Whereas IFN-alpha 2 is twice as active on human as on bovine cells, IFN-alpha 1 is 10 to 20 times more active on bovine than on human cells. As deduced from the cDNA's, the messenger RNA's for the two IFN's differ in length and in 20 percent of the nucleotides; the mature IFN polypeptides differ in 17 percent of the amino acids. Both IFN-alpha 1 and IFN-alpha 2 differ from the lymphoblastoid IFN described by others. Therefore, at least three different IFN-alpha genes are expressed in man; studies on genomic DNA reveal the presence of at least eight IFN-related genes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Streuli, M -- Nagata, S -- Weissmann, C -- New York, N.Y. -- Science. 1980 Sep 19;209(4463):1343-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6158094" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; Base Sequence ; DNA, Recombinant ; Escherichia coli/genetics ; Genes ; Humans ; *Interferons/genetics ; Leukocytes ; Lymphocytes ; Mice ; RNA, Messenger/genetics ; Structure-Activity Relationship
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    DNA methylation and gene function (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-11-07
    Description: In most higher organisms, DNA is modified after synthesis by the enzymatic conversion of many cytosine residues to 5-methylcytosine. For several years, control of gene activity by DNA methylation has been recognized as a logically attractive possibility, but experimental support has proved elusive. However, there is now reason to believe, from recent studies, that DNA methylation is a key element in the hierarchy of control mechanisms that govern vertebrate gene function and differentiation.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Razin, A -- Riggs, A D -- GM20483/GM/NIGMS NIH HHS/ -- GM25825/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1980 Nov 7;210(4470):604-10.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6254144" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Differentiation ; DNA/*physiology ; DNA (Cytosine-5-)-Methyltransferase/*metabolism ; DNA Restriction Enzymes/metabolism ; Deoxycytosine Nucleotides/*metabolism ; Deoxyribonucleoproteins/metabolism ; Gene Expression Regulation ; Methylation ; Methyltransferases/*metabolism ; Nucleosomes/ultrastructure ; Protein Binding ; Structure-Activity Relationship ; Substrate Specificity ; Tissue Distribution
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    War gases as olfactory probes (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-10-01
    Description: The tear gas ethyl bromoacetate is a fruity-smelling alkylating agent that blocks the ability of the frog nose to respond to esters and a variety of other odorants, but leaves sensitivity to amines unimpaired. Lachrymators and chemical warfare agents of other functional types such as sulfides (mustard gas) and amines (nitrogen mustards) may have similarly specific actions that will enable their use as chemical probes of the sense of smell.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Criswell, D W -- McClure, F L -- Schaefer, R -- Brower, K R -- New York, N.Y. -- Science. 1980 Oct;210(4468):425-6.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6968976" target="_blank"〉PubMed〈/a〉
    Keywords: Alkylating Agents/*pharmacology ; Amines ; Animals ; Chemical Warfare Agents/*pharmacology ; Esters ; Membrane Potentials/drug effects ; Rana pipiens ; Smell/*drug effects/physiology ; Structure-Activity Relationship
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    Calmodulin plays a pivotal role in cellular regulation (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-01-04
    Description: The role of calcium ions (Ca2+) in cell function is beginning to be unraveled at the molecular level as a result of recent research on calcium-binding proteins and particularly on calmodulin. These proteins interact reversibly with Ca2+ to form a protein . Ca2+ complex, whose activity is regulated by the cellular flux of Ca2+. Many of the effects of Ca2+ appear to be exerted through calmodulin-regulated enzymes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Cheung, W Y -- New York, N.Y. -- Science. 1980 Jan 4;207(4426):19-27.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6243188" target="_blank"〉PubMed〈/a〉
    Keywords: 3',5'-Cyclic-AMP Phosphodiesterases/metabolism ; Allosteric Regulation ; Amino Acid Sequence ; Animals ; Biological Evolution ; Calcium/*physiology ; Calcium-Binding Proteins/*physiology ; Calmodulin/*physiology ; Cell Communication ; Cyclic AMP/*physiology ; Enzyme Activation ; Phospholipases A/metabolism ; Protein Kinases/*metabolism ; Receptors, Drug/physiology ; Structure-Activity Relationship ; Troponin/physiology
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    Preferred sites of strand scission in DNA modified by andi-diol epoxide of benzo[a]pyrene (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-08-22
    Description: 〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Haseltine, W A -- Lo, K M -- D'Andrea, A D -- New York, N.Y. -- Science. 1980 Aug 22;209(4459):929-31.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7403858" target="_blank"〉PubMed〈/a〉
    Keywords: Base Sequence ; Benzopyrenes/*pharmacology ; Carcinogens ; *DNA, Bacterial ; Dose-Response Relationship, Drug ; Epoxy Compounds ; Hydrolysis ; Lac Operon ; Mutagens ; Stereoisomerism ; Structure-Activity Relationship
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    Pentobarbital: stereospecific actions of (+) and (-) isomers revealed on cultured mammalian neurons (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-01-11
    Description: Stereoisomers of the barbiturate anesthetic pentobarbital were applied to mouse spinal neurons growing in tissue culture. Intracellular recordings of neuronal membrane properties revealed that the (+) and (-) isomers caused direct changes in membrane potential and conductance on some but not all of the cells tested. The action of the (+) isomer was predominantly excitatory, whereas the (-) isomer produced predominantly inhibitory responses. The (-) isomer was considerably more effective in potentiating inhibitory responses to the transmitter gamma-aminobutyric acid. The results show that pentobarbital has multiple effects on neuronal excitability and demonstrate the presence of stereospecific sites of barbiturate action on central neurons.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Huang, L Y -- Barker, J L -- New York, N.Y. -- Science. 1980 Jan 11;207(4427):195-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7350656" target="_blank"〉PubMed〈/a〉
    Keywords: Action Potentials/drug effects ; Animals ; Cells, Cultured ; Dose-Response Relationship, Drug ; Electric Conductivity ; Membrane Potentials/drug effects ; Mice ; Neural Inhibition/drug effects ; Neurons/*drug effects ; Pentobarbital/*pharmacology ; Spinal Cord/embryology ; Stereoisomerism ; Structure-Activity Relationship
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    Anesthetics as teratogens: nitrous oxide is fetotoxic, xenon is not (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-11-21
    Description: Exposure of pregnant rats to the anesthetic nitrous oxide on the ninth day of gestation causes fetal resorption, skeletal anomalies, and macroscopic lesions including encephalocele, anophthalmia, microphthalmia, and gastroschisis. The inert gas xenon, which has anesthetic properties similar to those of nitrous oxide, does not cause teratogenic effects under the same experimental conditions.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Lane, G A -- Nahrwold, M L -- Tait, A R -- Taylor-Busch, M -- Cohen, P J -- Beaudoin, A R -- New York, N.Y. -- Science. 1980 Nov 21;210(4472):899-901.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7434002" target="_blank"〉PubMed〈/a〉
    Keywords: Anesthetics/*adverse effects ; Animals ; Female ; Nitrous Oxide/*toxicity ; Pregnancy ; Rats ; Structure-Activity Relationship ; *Teratogens ; Xenon/*toxicity
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    High-affinity [3H]imipramine binding in rat hypothalamus: association with uptake of serotonin but not of norepinephrine (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-12-05
    Description: Inhibition of the binding of [3H]imipramine and inhibition of the uptake of [3H]serotonin and [3H]norepinephrine by a series of antidepressants and other drugs were studied in the rat hypothalamus. No correlation was found between the potencies of these drugs for the inhibition of [3H]imipramine binding and the inhibition of [3H]norepinephrine uptake. There was, however, a highly significant correlation between the potencies of these drugs for the inhibition of [3H]serotonin uptake. These results suggest that high-affinity [3H]imipramine binding might be associated with the mechanism of serotonin uptake in the brain.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Langer, S Z -- Moret, C -- Raisman, R -- Dubocovich, M L -- Briley, M -- New York, N.Y. -- Science. 1980 Dec 5;210(4474):1133-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7444441" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Antidepressive Agents/pharmacology ; Biological Transport/drug effects ; *Carrier Proteins ; Hypothalamus/*metabolism ; Imipramine/*metabolism ; Norepinephrine/*metabolism ; Rats ; Receptors, Drug/*metabolism ; Serotonin/*metabolism ; Structure-Activity Relationship
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    N-Formylmethionyl peptide receptors on equine leukocytes initiate secretion but not chemotaxis (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-07-25
    Description: The chemotaxis of leukocytes appears to be initiated by the binding of chemotactic factors to the surface of these cells. N-Formylated peptides induce chemotaxis and lysosomal enzyme secretion of leukocytes; because these peptides are available in a purified radiolabeled form, they have been useful in the characterization of receptors for chemotactic factors. Equine polymorphonuclear leukocytes secrete lysosomal enzymes but do not exhibit chemotaxis in respone to the N-formylated peptides, even though they have a high-affinity cell surface receptor for these agents. The specificity of the equine receptor resembles the specificity of the receptor on chemotactically responsive leukocytes from other species. Equine polymorphonuclear leukocytes may thus be an excellent model for the study of the events that lead to a biological response following receptor occupancy.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Snyderman, R -- Pike, M C -- New York, N.Y. -- Science. 1980 Jul 25;209(4455):493-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6248959" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Chemotaxis ; Horses ; Kinetics ; Leukocytes/*physiology/secretion ; Oligopeptides/blood/*physiology ; Receptors, Cell Surface/*physiology ; Receptors, Formyl Peptide ; Structure-Activity Relationship
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    Cell growth with trans fatty acids is affected by adenosine 3',5'-monophosphate and membrane fluidity (1980)
    American Association for the Advancement of Science (AAAS)
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    Publication Date: 1980-02-15
    Description: Two positional isomers (9 and 11) of trans octadecenoates did not support growth on glucose of an Escherichia coli mutant that requires unsaturated fatty acids. However, the trans fatty acids provided sufficient fluidity to produce much higher cell yields when the concentration of adenosine 3',5'-monophosphate was raised. The effectiveness of the trans acids rose from 0 to 1 cell per femtomole to 15 to 20 cells per femtomole as the concentration of adenosine 3',5'-monophosphate was increased. The corresponding cis positional isomers supported high yields (35 to 40 cells per femtomole) independent of supplementation. The enhanced growth with adenosine 3',5'-monophosphate supplementation is not due to an increased uptake and incorporation of the trans isomers relative to the cis isomers, since the 9-trans isomer was incorporated more rapidly than the 9-cis isomer into the membrane phospholipids under all growth conditions and represented 21 +/- 2 mole percent of the acids. The finding that cells growing with trans fatty acid isomers have a higher requirement for adenosine 3',5'-monophosphate may indicate that some fatty acids can alter the metabolic regulation normally exerted by the cyclic nucleotide.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Tsao, Y K -- Lands, W E -- New York, N.Y. -- Science. 1980 Feb 15;207(4432):777-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6243419" target="_blank"〉PubMed〈/a〉
    Keywords: Cell Division ; Cyclic AMP/*metabolism ; Escherichia coli/*growth & development/metabolism ; Fatty Acids, Nonesterified/*physiology ; Isomerism ; *Membrane Fluidity ; Membrane Lipids/metabolism ; Structure-Activity Relationship
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    Mouse immunoglobulin D: messenger RNA and genomic DNA sequences (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-09-19
    Description: The molecular structure of a mouse immunoglobulin D from a plasmacytoma tumor and that of the normal mouse gene coding for immunoglobulin D are presented. The DNA sequence results indicate an unusual structure for the tumor delta chain in two respects: (i) Only two constant (C) region domains, termed C delta 1 and C delta 3 by homology considerations, are found; the two domains are separated by an unusual hinge region C delta H that lacks cysteine residues and thus cannot provide the covalent cross-links between heavy chains typically seen in immunoglobulins. The two domains and hinge are all coded on separate exons. (ii) At the carboxyl end of the delta chain there is a stretch of 26 amino acids that is coded from an exon located 2750 to 4600 base pairs downstream from the rest of the gene. Analogy with immunoglobulin M suggests that this distally coded segment C delta DC may have a membrane-binding function; however, it is only moderately hydrophobic. A fifth potential exon (C delta AC), located adjacent to the 3' (carboxyl) end of C delta 3, could code for a stretch of 49 amino acids. The tumor's expression of the delta gene may be aberrant, but the simplest interpretation would be that this tumor expresses one of the several biologically significant forms of the delta chain.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Tucker, P W -- Liu, C P -- Mushinski, J F -- Blattner, F R -- New York, N.Y. -- Science. 1980 Sep 19;209(4463):1353-60.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6968091" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Animals ; B-Lymphocytes/*immunology ; Base Sequence ; *Genes ; Glycoproteins/genetics ; Immunoglobulin Constant Regions/genetics ; Immunoglobulin D/*genetics ; Mice ; Myeloma Proteins/genetics ; RNA, Messenger/*genetics ; Receptors, Antigen, B-Cell/genetics ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 82
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    Prostaglandin A compounds as antiviral agents (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1980-08-29
    Description: Prostaglandins of the A series strongly inhibit the production of Sendai virus in African green monkey kidney cells and are able to prevent the establishment of persistent infection ("carrier" state). This action is specific for prostaglandin A and is not due to alteration in the host cell metabolism or in the virus infectivity. The possibility that this effect is mediated by interferon is discussed.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Santoro, M G -- Benedetto, A -- Carruba, G -- Garaci, E -- Jaffe, B M -- New York, N.Y. -- Science. 1980 Aug 29;209(4460):1032-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6157190" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arachidonic Acids/pharmacology ; Cell Line ; Dose-Response Relationship, Drug ; Haplorhini ; Interferons/pharmacology ; Parainfluenza Virus 1, Human/*drug effects ; Prostaglandins/pharmacology ; Prostaglandins A/*pharmacology ; Structure-Activity Relationship ; Thromboxanes/pharmacology ; Virus Replication/*drug effects
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 83
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    Site-specific mutagenesis of the human interleukin-2 gene: structure-function analysis of the cysteine residues (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-06-29
    Description: The gene encoding human interleukin-2 (IL-2) has been cloned from human spleen cells, peripheral blood lymphocytes, and the Jurkat cell line. Nucleotide sequence analysis of the gene revealed that the encoded IL-2 protein has three cysteines located at amino acid residues 58, 105, and 125 of the mature protein. Site-specific mutagenesis procedures were used to modify the IL-2 gene by changing each of the cysteine codons individually to serine codons. Substitution of serine for cysteine residues at either position 58 or 105 of the IL-2 protein substantially reduced biological activity, indicating that the cysteines at these positions are necessary for maintenance of the biologically active conformation and may therefore be linked by a disulfide bridge. The modified IL-2 protein containing a substitution at position 125 retained full biological activity, suggesting that the cysteine at this position is not involved in a disulfide bond and that a free sulfhydryl group at that position is not necessary for receptor binding.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Wang, A -- Lu, S D -- Mark, D F -- New York, N.Y. -- Science. 1984 Jun 29;224(4656):1431-3.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6427925" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Base Sequence ; Cell Line ; Cysteine/metabolism ; DNA, Recombinant/metabolism ; Escherichia coli/genetics ; Genes ; Humans ; Interleukin-2/*genetics ; *Mutation ; Receptors, Immunologic/metabolism ; Receptors, Interleukin-2 ; Serine/metabolism ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 84
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    A conformationally constrained vasopressin analog with antidiuretic antagonistic activity (1984)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1984-10-26
    Description: Application of information derived from a three-dimensional model of vasopressin bound to its antidiuretic receptor resulted in the design and synthesis of a bicyclic vasopressin analog, [5,8-cyclo(1-beta-mercaptopropionic acid,2-phenylalanine,5-aspartic acid,8-lysine)]vasopressin. The analog acts as an antagonist of the antidiuretic activity of vasopressin.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Skala, G -- Smith, C W -- Taylor, C J -- Ludens, J H -- New York, N.Y. -- Science. 1984 Oct 26;226(4673):443-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6541806" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Arginine Vasopressin/*analogs & derivatives ; Lypressin/*analogs & derivatives ; Male ; Rats ; Rats, Inbred Strains ; Structure-Activity Relationship
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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  • 85
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    Directed mutagenesis of dihydrofolate reductase (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1983-11-18
    Description: Three mutations of the enzyme dihydrofolate reductase were constructed by oligonucleotide-directed mutagenesis of the cloned Escherichia coli gene. The mutations--at residue 27, aspartic acid replaced with asparagine; at residue 39, proline replaced with cysteine; and at residue 95, glycine replaced with alanine--were designed to answer questions about the relations between molecular structure and function that were raised by the x-ray crystal structures. Properties of the mutant proteins show that Asp-27 is important for catalysis and that perturbation of the local structure at a conserved cis peptide bond following Gly-95 abolishes activity. Substitution of cysteine for proline at residue 39 results in the appearance of new forms of the enzyme that correspond to various oxidation states of the cysteine. One of these forms probably represents a species cross-linked by an intrachain disulfide bridge between the cysteine at position 85 and the new cysteine at position 39.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Villafranca, J E -- Howell, E E -- Voet, D H -- Strobel, M S -- Ogden, R C -- Abelson, J N -- Kraut, J -- CA17374/CA/NCI NIH HHS/ -- F32 GM09375/GM/NIGMS NIH HHS/ -- GM10928/GM/NIGMS NIH HHS/ -- New York, N.Y. -- Science. 1983 Nov 18;222(4625):782-8.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/6356360" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Base Sequence ; Disulfides ; Escherichia coli/genetics ; Gene Expression Regulation ; Genes ; Genes, Bacterial ; *Mutation ; Structure-Activity Relationship ; Tetrahydrofolate Dehydrogenase/*genetics
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
    Published by American Association for the Advancement of Science (AAAS)
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