A panel of cytochrome P450 BM3 variants to produce drug metabolites and diversify lead compounds

…, P Kulanthaivel, MS Kuo, H Hemmerle…

文献索引：Sawayama, Andrew M.; Chen, Michael M. Y.; Kulanthaivel, Palaniappan; Kuo, Ming-Shang; Hemmerle, Horst; Arnold, Frances H. Chemistry - A European Journal, 2009 , vol. 15, # 43 p. 11723 - 11729

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被引用次数: 90

摘要

Abstract Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one research compound. The most active enzymes support preparation of individual metabolites for preclinical bioactivity and toxicology evaluations. Underscoring their potential utility in ...