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人类细胞色素P450酶的催化选择性:与药物代谢和毒性的关系

Catalytic selectivity of human cytochrome P450 enzymes: relevance to drug metabolism and toxicity.

作者信息

Guengerich F P

机构信息

Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232-0146.

出版信息

Toxicol Lett. 1994 Feb 1;70(2):133-8. doi: 10.1016/0378-4274(94)90156-2.

DOI:10.1016/0378-4274(94)90156-2
PMID:8296317
Abstract

About 30 different human cytochrome P450 (P450) enzymes have now been characterized in considerable detail. It is possible to elucidate their catalytic specificities towards drugs, steroids, carcinogens, and other potential substrates with in vitro assays. It is also possible to ascertain the levels of individual P450 enzymes in humans with the use of drugs, after appropriate assay validation. The ability to discern catalytic selectivity and levels of P450 enzymes within individuals offers considerable potential in drug development, prevention of undesirable drug-drug interactions, and understanding the etiology of diseases resulting from exposure to potentially toxic and carcinogenic chemicals.

摘要

目前,已经对约30种不同的人类细胞色素P450(P450)酶进行了相当详细的表征。通过体外试验可以阐明它们对药物、类固醇、致癌物和其他潜在底物的催化特异性。在经过适当的试验验证后,使用药物也可以确定人体内个体P450酶的水平。辨别个体内P450酶的催化选择性和水平的能力在药物开发、预防不良药物相互作用以及理解接触潜在有毒和致癌化学物质导致的疾病病因方面具有巨大潜力。

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