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Article

Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates.

Chemical research in toxicology - 1 Dec 2007

Pearson Josh T, Wahlstrom Jan L, Dickmann Leslie J, Kumar Santosh, Halpert James R, Wienkers Larry C, Foti Robert S, Rock Dan A

Abstract excerpt

The role of C239 as the active-site residue responsible for forming the covalent linkage with raloxifene during P450 3A4 time-dependent inactivation (TDI) was recently identified. The corresponding residue in CYP3A5 is S239, and when the potential for TDI in P450 3A5 was investigated, only revers...

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Identifiers

PMID: 18001057
DOI: 10.1021/tx700207u

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026. Prepared record publication-18001057-2026-09-02.2. Manifest publication-graph-cohort-2026-09-02.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 2 Sept 2026.

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