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某些有机化合物对人碳酸酐酶II的抑制作用。

The inhibition of human carbonic anhydrase II by some organic compounds.

作者信息

Tibell L, Forsman C, Simonsson I, Lindskog S

出版信息

Biochim Biophys Acta. 1985 Jun 10;829(2):202-8. doi: 10.1016/0167-4838(85)90189-x.

DOI:10.1016/0167-4838(85)90189-x
PMID:3995052
Abstract

The inhibition of human carbonic anhydrase II (carbonate hydro-lyase, EC 4.2.1.1) by tetrazole, 1,2,4-triazole, 2-nitrophenol, and chloral hydrate has been investigated. These inhibitors, together with phenol which has been studied previously (Simonsson, I., Jonsson, B.-H. and Lindskog, S. (1982) Biochem. Biophys. Res. Commun. 108, 1406-1412), can be classified in three groups depending upon the kinetic patterns of inhibition of CO2 hydration at pH near 9. The first group, represented by tetrazole and 2-nitrophenol, yields predominantly uncompetitive inhibition under these conditions in analogy with simple, inorganic anions. The second group, represented by 1,2,4-triazole and chloral hydrate gives rise to essentially noncompetitive inhibition patterns, whereas phenol, representing the third group, is a competitive inhibitor of CO2 hydration. These diverse inhibition patterns are discussed in terms of the kinetic mechanism scheme originally proposed by Steiner et al. (Steiner, H., Jonsson, B.-H. and Lindskog, S. (1975) Eur. J. Biochem. 59, 253-259.

摘要

对四氮唑、1,2,4-三氮唑、2-硝基苯酚和水合氯醛对人碳酸酐酶II(碳酸水解酶,EC 4.2.1.1)的抑制作用进行了研究。这些抑制剂,连同之前已研究过的苯酚(Simonsson, I., Jonsson, B.-H. 和 Lindskog, S. (1982) Biochem. Biophys. Res. Commun. 108, 1406 - 1412),根据在pH接近9时对CO₂水合作用的抑制动力学模式可分为三组。第一组以四氮唑和2-硝基苯酚为代表,在这些条件下主要产生非竞争性抑制,类似于简单的无机阴离子。第二组以1,2,4-三氮唑和水合氯醛为代表,产生基本的非竞争性抑制模式,而代表第三组的苯酚是CO₂水合作用的竞争性抑制剂。根据Steiner等人最初提出的动力学机制方案(Steiner, H., Jonsson, B.-H. 和 Lindskog, S. (1975) Eur. J. Biochem. 59, 253 - 259)对这些不同的抑制模式进行了讨论。

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