Johnson Eric F, Stout C David
Department of Molecular and Experimental Medicine, The Scripps Research Institute, La Jolla, CA 92037, USA.
Biochem Biophys Res Commun. 2005 Dec 9;338(1):331-6. doi: 10.1016/j.bbrc.2005.08.190. Epub 2005 Sep 2.
Cytochrome P450 monooxygenases provide important pathways for the metabolic clearance of drugs and toxins in humans. These enzymes are expressed from multiple genes and exhibit complex patterns of differential and overlapping substrate selectivity. Recent structures of microsomal P450s determined by X-ray crystallography have provided a structural basis for understanding differences in substrate recognition. This review will describe similarities and differences in the active site structures of four human microsomal cytochrome P450 monooxygenases, 2A6, 2C8, 2C9, and 3A4, that contribute extensively to drug and toxin metabolism.
细胞色素P450单加氧酶为人体中药物和毒素的代谢清除提供了重要途径。这些酶由多个基因表达，并表现出复杂的底物选择性差异和重叠模式。最近通过X射线晶体学确定的微粒体P450的结构为理解底物识别差异提供了结构基础。本综述将描述四种对药物和毒素代谢有广泛贡献的人微粒体细胞色素P450单加氧酶2A6、2C8、2C9和3A4的活性位点结构的异同。
