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前列腺素环氧化酶受体位点的构象要求:设计非甾体抗炎药的模板。

Conformational requirements at the prostaglandin cyclooxygenase receptor site: a template for designing non-steroidal anti-inflammatory drugs.

作者信息

Appleton R A, Brown K

出版信息

Prostaglandins. 1979 Jul;18(1):29-34. doi: 10.1016/s0090-6980(79)80020-9.

DOI:10.1016/s0090-6980(79)80020-9
PMID:118488
Abstract

When space-filling models of the peroxy radical precursor of PGG were compared with models of 2(S)-(3-chloro-4-cyclohexylphenyl) propionic acid and other acidic cyclooxygenase inhibitors several common structural features were revealed. This led us to propose a template for designing non-steroidal anti-inflammatory drugs (NSAID's) based on the conformation of the peroxy radical immediately prior to its cyclisation to PGG. The template can be equated with a complementary cyclooxygenase receptor site.

摘要

当将PGG过氧自由基前体的空间填充模型与2(S)-(3-氯-4-环己基苯基)丙酸及其他酸性环氧化酶抑制剂的模型进行比较时,发现了几个共同的结构特征。这使我们基于过氧自由基环化形成PGG之前的构象,提出了一种设计非甾体抗炎药(NSAID)的模板。该模板可等同于一个互补的环氧化酶受体位点。

相似文献

1
Conformational requirements at the prostaglandin cyclooxygenase receptor site: a template for designing non-steroidal anti-inflammatory drugs.前列腺素环氧化酶受体位点的构象要求:设计非甾体抗炎药的模板。
Prostaglandins. 1979 Jul;18(1):29-34. doi: 10.1016/s0090-6980(79)80020-9.
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Conformational requirements at the prostaglandin cyclooxygenase receptor site.前列腺素环氧化酶受体位点的构象要求。
Agents Actions Suppl. 1979(4):188-92.
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A model for the prostaglandin synthetase cyclooxygenation site and its inhibition by antiinflammatory arylacetic acids.前列腺素合成酶环氧化位点模型及其被抗炎芳基乙酸抑制的作用
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Structural characterization of a pentadienyl radical intermediate formed during catalysis by prostaglandin H synthase-2.
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Inhibitors of cyclooxygenase and a receptor-site model for cyclooxygenase.环氧化酶抑制剂与环氧化酶的受体位点模型
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The cyclooxygenase isoforms: structural insights into the conversion of arachidonic acid to prostaglandins.环氧化酶同工型:对花生四烯酸转化为前列腺素的结构见解。
Biochim Biophys Acta. 1999 Nov 23;1441(2-3):278-87. doi: 10.1016/s1388-1981(99)00147-x.
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Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents.抗炎药物对环氧合酶-2选择性抑制的结构基础。
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COX in a crystal ball: current status and future promise of prostaglandin research.前列腺素研究的现状与未来前景:COX的预测
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The structure of mammalian cyclooxygenases.哺乳动物环氧化酶的结构。
Annu Rev Biophys Biomol Struct. 2003;32:183-206. doi: 10.1146/annurev.biophys.32.110601.141906. Epub 2003 Feb 5.

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J Comput Aided Mol Des. 1993 Apr;7(2):183-98. doi: 10.1007/BF00126444.
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Nonsteroidal anti-inflammatory drugs in perisurgical pain management. Mechanisms of action and rationale for optimum use.围手术期疼痛管理中的非甾体类抗炎药。作用机制及最佳使用原理。
Drugs. 1995 Jan;49(1):51-70. doi: 10.2165/00003495-199549010-00005.
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Effects of inflammatory agents on endothelial lysosomal fragility and their inhibition by anti-inflammatory drugs.
炎症因子对内皮细胞溶酶体脆性的影响及其被抗炎药物的抑制作用。
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Inhibition of a major NAD(P)-linked oxidoreductase from rat liver cytosol by steroidal and nonsteroidal anti-inflammatory agents and by prostaglandins.甾体和非甾体抗炎药以及前列腺素对大鼠肝细胞溶胶中一种主要的NAD(P)连接氧化还原酶的抑制作用。
Proc Natl Acad Sci U S A. 1983 Jul;80(14):4504-8. doi: 10.1073/pnas.80.14.4504.