Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.
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ABSTRACT:
SUBMITTER: Wright WC
PROVIDER: S-EPMC7087482 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
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Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.
Wright William C WC Chenge Jude J Wang Jingheng J Girvan Hazel M HM Yang Lei L Chai Sergio C SC Huber Andrew D AD Wu Jing J Oladimeji Peter O PO Munro Andrew W AW Chen Taosheng T
Journal of medicinal chemistry 20200122 3
The human cytochrome P450 (CYP) enzymes CYP3A4 and CYP3A5 metabolize most drugs and have high similarities in their structure and substrate preference. Whereas CYP3A4 is predominantly expressed in the liver, CYP3A5 is upregulated in cancer, contributing to drug resistance. Selective inhibitors of CYP3A5 are, therefore, critical to validating it as a therapeutic target. Here we report clobetasol propionate (clobetasol) as a potent and selective CYP3A5 inhibitor identified by high-throughput scree ...[more]
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