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  • Structure-Activity Relationship  (36)
  • American Association for the Advancement of Science (AAAS)  (36)
  • American Geophysical Union
  • Periodicals Archive Online (PAO)
  • Springer Nature
  • 1980-1984  (36)
  • 1925-1929
  • 1983  (14)
  • 1980  (22)
  • 1926
Collection
Keywords
Publisher
  • American Association for the Advancement of Science (AAAS)  (36)
  • American Geophysical Union
  • Periodicals Archive Online (PAO)
  • Springer Nature
Years
  • 1980-1984  (36)
  • 1925-1929
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
    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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  • 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
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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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
    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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  • 6
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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
    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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  • 7
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    Antibodies that react with predetermined sites on proteins (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 8
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    Monoclonal antibodies reveal the structural basis of antibody diversity (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 9
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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
    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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  • 10
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    Carbocyclic arabinofuranosyladenine (cyclaradine): efficacy against genital herpes in guinea pigs (1983)
    American Association for the Advancement of Science (AAAS)
    Details
    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
    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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  • 11
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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
    Print ISSN: 0036-8075
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  • 12
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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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  • 13
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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)
    Details
    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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  • 14
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    Tumor-promoting phorbol esters stimulate hematopoietic colony formation in vitro (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    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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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 15
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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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  • 16
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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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  • 17
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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)
    Details
    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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  • 18
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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)
    Details
    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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  • 19
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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)
    Details
    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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  • 20
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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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  • 21
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    Asymmetry of the acetylcholine channel revealed by quaternary anesthetics (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 22
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    Angiotoxicity of oxygenated sterols and possible precursors (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 23
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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)
    Details
    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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  • 24
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    At least three human type alpha interferons: structure of alpha 2 (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 25
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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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  • 26
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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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  • 27
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    Calmodulin plays a pivotal role in cellular regulation (1980)
    American Association for the Advancement of Science (AAAS)
    Details
    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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  • 28
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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)
    Details
    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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  • 29
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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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  • 30
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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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  • 31
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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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    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 32
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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)
    Details
    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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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 33
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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)
    Details
    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
    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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  • 34
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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
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 35
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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
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  • 36
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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
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    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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