Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development

• Published in: Current medicinal chemistry Vol. 16; no. 27; p. 3480
• Main Authors: Zhou, Shu-Feng, Zhou, Zhi-Wei, Yang, Li-Ping, Cai, Jian-Ping
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01.09.2009
• Subjects: Aryl Hydrocarbon Hydroxylases - antagonists & inhibitors; Aryl Hydrocarbon Hydroxylases - genetics; Aryl Hydrocarbon Hydroxylases - metabolism; Catalytic Domain; Chromosomes, Human, Pair 10; Cytochrome P-450 CYP2C9; Cytochrome P-450 Enzyme System - genetics; Cytochrome P-450 Enzyme System - metabolism; Drug Discovery; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Humans; Receptors, Cytoplasmic and Nuclear - metabolism; Structure-Activity Relationship; Substrate Specificity

Cytochrome P450 2C9 (CYP2C9) is one of the most abundant CYP enzymes in the human liver. CYP2C9 metabolizes more than 100 therapeutic drugs, including tolbutamide, glyburide, diclofenac, celecoxib, torasemide, phenytoin losartan, and S-warfarin). Some natural and herbal compounds are also metabolize...