Title : Mechanism-based inactivation of human cytochrome P450 2B6 by clopidogrel: involvement of both covalent modification of cysteinyl residue 475 and loss of heme.

Pub. Date : 2011 Nov

PMID : 21862689






3 Functional Relationships(s)
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1 Mechanism-based inactivation of human cytochrome P450 2B6 by clopidogrel: involvement of both covalent modification of cysteinyl residue 475 and loss of heme. Heme cytochrome P450 family 2 subfamily B member 6 Homo sapiens
2 Furthermore, inactivation of both CYP2B6 WT and C475S by clopidogrel, but not by 2-oxo-clopidogrel, led to the loss of the heme, which accounts for most of the loss of the catalytic activity. Heme cytochrome P450 family 2 subfamily B member 6 Homo sapiens
3 Collectively, these results suggest that clopidogrel inactivates CYP2B6 primarily through destruction of the heme, whereas 2-oxo-clopidogrel inactivates CYP2B6 through covalent modification of Cys475. Heme cytochrome P450 family 2 subfamily B member 6 Homo sapiens