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细胞色素P450与药物发现

Cytochromes P450 and drug discovery.

作者信息

Lamb David C, Waterman Michael R, Kelly Steven L, Guengerich F Peter

机构信息

Institute of Life Science, Swansea Medical School, Grove Building, Swansea University, Swansea SA2 8PP, UK.

出版信息

Curr Opin Biotechnol. 2007 Dec;18(6):504-12. doi: 10.1016/j.copbio.2007.09.010. Epub 2007 Nov 19.

Abstract

Cytochromes P450 (CYP) are a superfamily of haem-containing proteins distributed widely throughout nature. Historically, they have a central role in drug metabolism and following the advent of genomics they have been shown to have key roles in the biosynthesis of natural products which are used as medicines. Herein, we provide an overview of CYP systems with particular emphasis on their role as drug targets, their involvement in drug biosynthesis and potential strategies for developing new derivatives of drugs based on CYP engineering. The applied importance of CYPs for medicinal and biotechnological applications will also be discussed.

摘要

细胞色素P450(CYP)是一类含血红素的蛋白质超家族,广泛分布于自然界。从历史上看,它们在药物代谢中起着核心作用,随着基因组学的出现,已证明它们在用作药物的天然产物的生物合成中起关键作用。在此,我们概述了CYP系统,特别强调它们作为药物靶点的作用、它们在药物生物合成中的参与以及基于CYP工程开发药物新衍生物的潜在策略。还将讨论CYPs在医学和生物技术应用中的应用重要性。

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