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Article

Analysis of homotropic and heterotropic cooperativity of diazepam oxidation by CYP3A4 using site-directed mutagenesis and kinetic modeling.

Archives of biochemistry and biophysics - 1 Jan 2003

He You Ai, Roussel Fabienne, Halpert James R

Abstract excerpt

The structural basis for the cooperativity of diazepam oxidation catalyzed by human cytochrome P450 3A4 (CYP3A4) and 40 mutants has been investigated. An ordered two-site model in which substrates bind first to a catalytic/effector site and then to the catalytic site was used to explain sigmoidal kinetics for temazepam formation but hyperbolic kinetics for nordiazepam formation. In this model diazepam binds to...

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Source

Identifiers

PMID: 12464248
DOI: 10.1016/s0003-9861(02)00484-8

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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