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  • Articles  (35)
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  • Latest Papers from Table of Contents or Articles in Press  (35)
  • Structure-Activity Relationship  (35)
  • 1975-1979  (35)
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  • Latest Papers from Table of Contents or Articles in Press  (35)
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  • 1
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    A structural model for the kinetic behavior of hemoglobin (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-11-30
    Description: The tertiary structures of all liganded hemoglobins in the R state differ in detail. Steric hindrance arising from nonbonded ligand-globin interactions affects the binding of ligands such as CO and cyanide which preferentially form linear axial complexes to heme; these ligands bind in a strained off-axis configuration. Ligands such as O2 and NO, which preferentially form bent complexes, encounter less steric hindrance and can bind in their (preferred) unstrained configuration. Linear complexes distort the ligand pockets in the R state (and by inference, in the T state) more than bent complexes. These structural differences between linear and bent complexes are reflected in the kinetic behavior of hemoglobin. Structural interpretation of this kinetic behavior indicates that the relative contributions of nonbonded ligand-globin interactions and nonbonded heme interactions to transition state free energies differ for linear and bent ligands. The relative contributions of these interactions to the free energy of cooperativity may also differ for linear and bent ligands. Thus the detailed molecular mechanism by which the affinity of heme is regulated differs for different ligands.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Moffat, K -- Deatherage, J F -- Seybert, D W -- New York, N.Y. -- Science. 1979 Nov 30;206(4422):1035-42.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/493990" target="_blank"〉PubMed〈/a〉
    Keywords: Allosteric Regulation ; Animals ; Heme/*metabolism ; Hemoglobins/metabolism ; Horses ; Kinetics ; Ligands ; Oxygen/*metabolism ; Oxyhemoglobins/*metabolism ; Protein Conformation ; Stereoisomerism ; 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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  • 2
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    Elimination of metabolic cooperation in Chinese hamster cells by a tumor promoter (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-11-30
    Description: Wild-type Chinese hamster V79 cells (6-thioguanine-sensitive) reduce the recovery of 6-thioguanine-resistant cells when they are cultured together at high densities, through a form of intercellular communication (metabolic cooperation). Cooperation is inhibited by 12-O-tetradecanoyl phorbol-13-acetate, rescuing the 6-thioguanine-resistant cells. These results may be useful in the study of an aspect of the mechanism of tumor promotion and in assaying for promoters.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Yotti, L P -- Chang, C C -- Trosko, J E -- New York, N.Y. -- Science. 1979 Nov 30;206(4422):1089-91.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/493994" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Cell Communication/*drug effects ; Cell Membrane/drug effects ; Cricetinae ; Dose-Response Relationship, Drug ; Drug Resistance ; Phorbol Esters/*pharmacology ; Phorbols/*pharmacology ; Structure-Activity Relationship ; Tetradecanoylphorbol Acetate/pharmacology ; Thioguanine/pharmacology
    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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    Differential competition with cytotoxic agents: an approach to selectivity in cancer chemotherapy (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-11-30
    Description: An approach to increasing the selectivity of cancer chemotherapeutic agents is presented in which noncytotoxic competitive substrates are used to discern the differences in structural requirements for transport of cytotoxic agents between tumor cells and a sensitive host tissue, the hematopoietic precursor cells of the bone marrow. Examples are given for two such systems, one responsible for the transport of nucleosides and another for the transport of amino acids. Cytidine is twice as effective in reducing the toxicity of showdomycin for murine bone marrow cells in culture as it is for murine L1210 leukemia cella. Conversely, homoleucine is twice as effective in reducing the toxicity of melphalan for L1210 cells as it is for bone marrow cells. These observations can serve as a basis for the development of bone marrow protective agents and for the design of cytotoxic agents that may be preferentially transported into tumor cells.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Rabinowitz, M -- Uehara, Y -- Vistica, D T -- New York, N.Y. -- Science. 1979 Nov 30;206(4422):1085-7.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/493993" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Antibiotics, Antineoplastic/*metabolism ; Biological Transport ; Bone Marrow/drug effects ; Leukemia L1210/drug therapy ; Melphalan/metabolism/therapeutic use ; Mice ; Neoplasms/*drug therapy ; Showdomycin/*metabolism/therapeutic use ; 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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    Heparin: an old drug with a new paradigm (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-11-02
    Description: Recent studies have shown that heparin is a biochemical representative of a distinct class of compounds known as linear anionic polyelectrolytes. Members of this class are mixtures of individual highly negatively charged chains that show a wide spectrum of specific reactions with biologically active proteins. Upon administration, heparin chains enter a cellular pool and effectively prevent thrombosis by increasing the electronegative potential of the vessel wall. Anticoagulant activity is an unusual feature of a few heparin chains and appears to play a minor role in many clinical uses and in physiological and pathological responses.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Jacques, L B -- New York, N.Y. -- Science. 1979 Nov 2;206(4418):528-33.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/386509" target="_blank"〉PubMed〈/a〉
    Keywords: Antithrombin III/metabolism ; Blood Coagulation/drug effects ; Heparin/adverse effects/*pharmacology/therapeutic use ; Humans ; Ions ; Mast Cells/physiology ; Structure-Activity Relationship ; Sulfates/metabolism ; Thrombosis/prevention & control
    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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  • 5
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    Heterogeneity of vertebrate luteinizing hormone-releasing hormone (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-10-05
    Description: Radioimmunoassay and chromatography analyses of hypothalamic luteinizing hormone-releasing hormone (LHRH) have demonstrated the presence of LHRH-like immunoreactive peptides in a wide range of vertebrates. Contrary to previous reports, the molecule differs in various vertebrates. Avian, reptilian, and teleostean LHRH's are chemically distinct from the mammalian peptide but are in themselves indistinguishable. However, amphibian LHRH appears to be identical to the mammalian peptide. These findings have interesting evolutionary implications.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉King, J A -- Millar, R P -- New York, N.Y. -- Science. 1979 Oct 5;206(4414):67-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/384514" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; *Biological Evolution ; Chromatography ; Gonadotropin-Releasing Hormone/*analysis/immunology ; Hypothalamus/analysis ; Radioimmunoassay ; 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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  • 6
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    Sporozoite-induced malaria: therapeutic effects of glycolipids in liposomes (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-09-14
    Description: Liposomes containing neutral glycolipids with a terminal glucose or galactose, when injected intravenously, prevented the appearance of erythrocytic forms of malaria (Plasmodium berghei) in mice previously injected with sporozoites. Inhibitory glycolipids included glucosyl, galactosyl, or lactosyl ceramide. Inhibition was not observed with liposomes containing ceramide, phosphocholine ceramide, sulfogalactosyl ceramide (sulfatide), or ganglioside GM1. Liposomes containing glycolipids did not inhibit infection transmitted by injecting blood containing erythrocytic stages of malaria. These results may have therapeutic implications in the treatment of malaria. Analysis of the mechanism of interference with the life cycle of malaria by liposomal glycolipids may yield information about the interactions of parasites with cellular membranes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Alving, C R -- Schneider, I -- Swartz, G M Jr -- Steck, E A -- New York, N.Y. -- Science. 1979 Sep 14;205(4411):1142-4.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/382358" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Ceramides/therapeutic use ; Erythrocytes/parasitology ; Glycolipids/*therapeutic use ; Liposomes/therapeutic use ; Liver/parasitology ; Malaria/parasitology/*therapy ; Mice ; Plasmodium berghei ; 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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    Comparative biochemistry and drug design for infectious disease (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-09-07
    Description: In the past two decades, biochemistry and molecular biology have demonstrated the existence of potentially exploitable biochemical differences between etiologic agents of disease and their hosts. Known differences between organism and host with respect to metabolism and polymer structure point to the detailed characterization of key proteins as the focus for the development of potential inhibitors. In the last decade, the methodology of the isolation, characterization, and inactivation of proteins and enzymes has been advanced. The present scientific and technological base suggests that new efforts toward the development of selective chemotherapeutic agents for infections caused by bacteria, viruses, protozoa, and higher eukaryotes should exploit the known differences in proteins or other specific biopolymers serving crucial structural or metabolic roles in the economy of the parasite.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Cohen, S S -- New York, N.Y. -- Science. 1979 Sep 7;205(4410):964-71.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/382357" target="_blank"〉PubMed〈/a〉
    Keywords: *Anti-Bacterial Agents ; *Antiviral Agents ; Communicable Diseases/*drug therapy ; Humans ; Mycobacterium leprae/metabolism ; Polysaccharides, Bacterial/metabolism ; Species Specificity ; Structure-Activity Relationship ; Trypanosomiasis/drug therapy ; Vidarabine/pharmacology ; Viral Proteins/biosynthesis ; 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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  • 8
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    Specific nonopiate receptors for beta-endorphin (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-09-07
    Description: Iodinated beta H-[2-D-alanine]endorphin exhibits specific binding to cultured human lymphocytes. The binding is inhibited by low concentrations of beta-endorphin and its D-alanine derivative, but is not affected by opiate agonists and antagonists, or by enkephalin analogs, beta-lipotropin, adrenocorticotrophic hormone, or alpha-melanocyte-stimulating hormone; this suggests the existence of a specific, non-opiate binding site (receptor) for beta-endorphin. The carboxy-terminal region of beta-endorphin is essential for this binding activity, since alpha-endorphin is not active. beta-Endorphin may be a circulating hormone with peripheral physiological effects that are not primarily mediated through interactions with opiate or enkephalin receptors.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Hazum, E -- Chang, K J -- Cuatrecasas, P -- New York, N.Y. -- Science. 1979 Sep 7;205(4410):1033-5.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/224457" target="_blank"〉PubMed〈/a〉
    Keywords: Amino Acid Sequence ; Cells, Cultured ; Endorphins/blood/*metabolism ; Humans ; Lymphocyte Activation ; Lymphocytes/*metabolism ; Receptors, Drug/*metabolism ; Receptors, Opioid/metabolism ; Stress, Physiological/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
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  • 9
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    Genetic effects of impure and pure saccharin in yeast (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-09-07
    Description: Yeast cells were grown in media containing impure or purified saccharin preparations. Dose-dependent increases in frequencies of cells possessing aberrant cell morphologies were revealed by light microscopy. At each test dose, cells grown in impure saccharin exhibited up to sevenfold higher frequencies of mitotic crossing-over or gene conversion in three of four assays for genetic recombination than cells grown in purified saccharin from the same lot. With one exception, the sweetener produced by the Maumee process caused larger increases in recombination and gene reversion than the sweetener produced by the Remsen-Fahlberg process. The several test markers did not respond equally to any test saccharin. Cells grown in liquid media containing no saccharin or two of three test concentrations of saccharin produced cell titers that were approximately equivalent.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Moore, C W -- Schmick, A -- New York, N.Y. -- Science. 1979 Sep 7;205(4410):1007-10.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/382356" target="_blank"〉PubMed〈/a〉
    Keywords: Cell Division/drug effects ; Crossing Over, Genetic/drug effects ; Dose-Response Relationship, Drug ; Mitosis/drug effects ; *Mutagens ; Recombination, Genetic/drug effects ; Saccharin/chemical synthesis/*pharmacology ; Saccharomyces cerevisiae/*drug effects ; 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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  • 10
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    Digitalis genin activity: side-group carbonyl oxygen position is a major determinant (1979)
    American Association for the Advancement of Science (AAAS)
    Details
    Publication Date: 1979-08-31
    Description: The Na+,k+-adenosine triphosphatase-inhibiting activity of digitalis genins and their analogs is a function of side-group carbonyl (C = O) oxygen position. For each 2.2 angstroms that this oxygen is displaced from its position in digitoxigenin, activity drops by one order of magnitude. This quantitative relation resolves previously proposed models which have attempted to describe the molecular basis of genin activity. A multidisciplinary (crystallographic, conformational energy, synthetic, biological) approach to structure-activity relations is described.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Fullerton, D S -- Yoshioka, K -- Rohrer, D C -- From, A H -- Ahmed, K -- New York, N.Y. -- Science. 1979 Aug 31;205(4409):917-9.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/224455" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Brain/enzymology ; Digitalis Glycosides/*pharmacology ; Molecular Conformation ; Rats ; Sodium-Potassium-Exchanging ATPase/*antagonists & inhibitors ; 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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