With the widespread use of O-alkoxyresorufin dealkylation assays since the 1990s,
thousands of inhibitors of cytochrome P450 family 1 enzymes (P450s 1A1, 1A2, and 1B1) …

Human cytochrome P450 1A2 (CYP1A2) is one of the major CYPs in the liver (&sim13%)
and metabolizes about 20% of clinically used drugs. CYP1A2 is a 515-residue protein with a …

The early detection of potential drug‐drug interactions is an important issue of drug
discovery that has led to the development of high‐throughput screening (HTS) methods for …

To discover new selective mechanism-based P450 inhibitors, eight 7-ethynylcoumarin
derivatives were prepared through a facile two-step synthetic route. Cytochrome P450 …

The balance between detoxification and bioactivation of a compound in a particular species
or organ is highly dependent on the relative amounts and activities of the different forms of …

Human cytochrome P450 (P450) enzymes exhibit remarkable diversity in their substrate
specificities, participating in oxidation reactions of a wide range of xenobiotic drugs …

Cytochromes P450 (CYPs) play an important role in the metabolism of endogenic and
xenobiotic substances, especially drugs. In addition, many CYPs may serve as targets for …

A series of 3-heteroaromatic analogues of nicotine were synthesized to delineate structural
and mechanistic requirements for selectively inhibiting human cytochrome P450 (CYP) 2A6 …

Key residue Val-382 in P450 1A1 has been predicted to interact with the alkoxy chain of
resorufin derivatives. Therefore, we undertook a detailed analysis of substrate mobility in the …

The US Food and Drug Administration (FDA) lists 22 medications as clinical inhibitors of
cytochrome P450 2D6 isoenzyme, with classifications of strong, moderate, and weak. It is …