Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2

P Lafite, S Dijols, D Buisson, AC Macherey…

文献索引：Lafite, Pierre; Dijols, Sylvie; Buisson, Didier; Macherey, Anne-Christine; Zeldin, Darryl C.; Dansette, Patrick M.; Mansuy, Daniel Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2777 - 2780

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被引用次数: 41

摘要

The active site topology, substrate specificity, and biological roles of the human cytochrome P450 CYP2J2, which is mainly expressed in the cardiovascular system, are poorly known even though recent data suggest that it could be a novel biomarker and potential target for therapy of human cancer. This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with Ki values as low as 160nM, that should be ...