tert-Butylphenylacetylene Is a Potent Mechanism-Based Inactivator of Cytochrome P450 2B4: Inhibition of Cytochrome P450 Catalysis by Steric Hindrance

We have demonstrated that 4-(tert-butyl)-phenylacetylene (tBPA) is a potent mechanism-based inactivator for cytochrome P450 2B4 (P450 2B4) in the reconstituted system. It inactivates P450 2B4 in a NADPH- and time-dependent manner with a K(I) of 0.44 μM and k(inact) of 0.12 min(−1). The partition rat...

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Main Authors: Zhang, Haoming, Lin, Hsia-lien, Walker, Vyvyca J., Hamdane, Djemel, Hollenberg, Paul F.
Format: Artigo
Language:Inglês
Published: The American Society for Pharmacology and Experimental Therapeutics 2009
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC2774989/
https://ncbi.nlm.nih.gov/pubmed/19720728
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/mol.109.059808
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