2024
DOI: 10.1021/acs.jcim.3c01837
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Probe Substrate Dependencies in CYP3A4 Allosteric Inhibition: A Novel Molecular Mechanism Involving F–F′ Loop Perturbations

Wan Wei,
Lloyd Wei Tat Tang,
Ravi Kumar Verma
et al.

Abstract: The biochemical basis for substrate dependences in apparent inhibition constant values (K i ) remains unknown. Our study aims to elucidate plausible structural determinants underpinning these observations. In vitro steady-state inhibition assays conducted using human recombinant CYP3A4 enzyme and testosterone substrate revealed that fibroblast growth factor receptor (FGFR) inhibitors erdafitinib and pemigatinib noncompetitively inhibited CYP3A4 with apparent K i values of 10.2 ± 1.1 and 3.3 ± 0.9 μM, respectiv… Show more

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