Wrighton S A, VandenBranden M, Ring B J
Department of Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.
J Pharmacokinet Biopharm. 1996 Oct;24(5):461-73. doi: 10.1007/BF02353474.
The superfamily of heme-thiolate proteins known as the cytochromes P450 is responsible for the oxidative metabolism of the majority of drugs. Thus, the phenotypes of individuals with respect to their levels of catalytically active cytochromes P450 determines to a large part the substantial interindividual variation observed in the metabolic clearance of drugs. Over the past 10 years 15 different human cytochromes P450 involved in drug metabolism have been isolated and characterized to varying degrees. This brief review discusses the characterization of these cytochromes P450 and how this knowledge has been used by the pharmaceutical industry to aid in the development of new drugs.
被称为细胞色素P450的血红素硫醇盐蛋白超家族负责大多数药物的氧化代谢。因此,个体催化活性细胞色素P450水平的表型在很大程度上决定了药物代谢清除中观察到的个体间显著差异。在过去10年里,已分离出15种参与药物代谢的不同人类细胞色素P450,并对其进行了不同程度的表征。这篇简短的综述讨论了这些细胞色素P450的表征,以及制药行业如何利用这些知识来辅助新药开发。