Ute M. Kent

TL;DR: Silybin was a potent inhibitor of UGT1A1 and was 14- and 20-fold more selective for UGT 1A1 than for U GT1A9 and UGT2A6, respectively, and careful administration of silybin with drugs primarily cleared by P450s 3A4 or 2C9 is advised, since drug-drug interactions cannot be excluded.

TL;DR: The P450 type cytochromes are responsible for the metabolism of a wide variety of xenobiotics and endogenous compounds and have the potential for causing serious drug-drug interactions that may have severe toxicological effects.

TL;DR: High-performance liquid chromatography analysis of the P450 heme confirmed that incubations with glabridin and NADPH did not result in the destruction of the heme moiety, and Heme and reduced CO spectral analysis indicated that glabridgein inactivated P450s 2B6 and 3A4 by different mechanisms.

TL;DR: The results demonstrate that EE is an effective mechanism-based inactivator of P450 3A4 and that the mechanism of inactivation involves not only heme destruction, but also the irreversible modification of the apoprotein at the active site.

TL;DR: A sampling of the types of studies that can be conducted using mechanism-based inactivators and highlight studies with several classes of compounds including acetylenes, isothiocyanates, xanthates, aminobenzotriazoles, phencyclidine, and furanocoumarins are presented.