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Thr302 Is the Site for the Covalent Modification of Human Cytochrome P450 2B6 Leading to Mechanism-Based Inactivation by tert-Butylphenylacetylene

The mechanism-based inactivation of human CYP2B6 by tert-butylphenylacetylene (BPA) in the reconstituted system was investigated. The inactivation of CYP2B6 by BPA is time-, concentration-, and NADPH-dependent and exhibits a K(I) of 2.8 μM, a k(inact) of 0.7 min(−1), and a t(1/2) of 1 min. The parti...

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Main Authors: Lin, Hsia-lien, Zhang, Haoming, Pratt-Hyatt, Matthew J., Hollenberg, Paul F.
Format: Artigo
Jezik:Inglês
Izdano: The American Society for Pharmacology and Experimental Therapeutics 2011
Teme:
Online dostop:https://ncbi.nlm.nih.gov/pmc/articles/PMC3226372/
https://ncbi.nlm.nih.gov/pubmed/21930824
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/dmd.111.042176
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