Modulation of P450 CYP3A4-dependent metabolism by P-glycoprotein: implications for P450 phenotyping.

Abstract excerpt

Some compounds used for phenotyping of cytochrome P450s are substrates of P-glycoprotein (pgp). It is likely that in these cases, the level of pgp modulates the metabolism of in vivo probes. To address this important issue, we have analyzed the effects of pgp on CYP3A4-mediated reactions in two newly established cell lines (3A4/HR/MDR(-) and 3A4/HR/MDR(+)), which express CYP3A4 in the absence and presence of pgp,...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to ATP Binding Cassette Transporter, Subfamily B, Member 1
• Share to Cardiotonic Agents