Title : Molecular Basis of Metabolism-Mediated Conversion of PK11195 from an Antagonist to an Agonist of the Constitutive Androstane Receptor.

Pub. Date : 2017 Jul

PMID : 28442602






1 Functional Relationships(s)
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1 Utilizing a HPH-HepG2 coculture model, we demonstrate that inclusion of HPH converts PK11195 from an antagonist to an agonist of hCAR, and such conversion was attenuated by potent CYP3A4 inhibitor ketoconazole. Ketoconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens