Correlating structure and function of drug-metabolizing enzymes: progress and ongoing challenges.

ABSTRACT: This report summarizes a symposium sponsored by the American Society for Pharmacology and Experimental Therapeutics at Experimental Biology held April 20-24 in Boston, MA. Presentations discussed the status of cytochrome P450 (P450) knowledge, emphasizing advances and challenges in relating structure with function and in applying this information to drug design. First, at least one structure of most major human drug-metabolizing P450 enzymes is known. However, the flexibility of these active sites can limit the predictive value of one structure for other ligands. A second limitation is our coarse-grain understanding of P450 interactions with membranes, other P450 enzymes, NADPH-cytochrome P450 reductase, and cytochrome b5. Recent work has examined differential P450 interactions with reduct

SUBMITTER: Johnson EF 

PROVIDER: S-EPMC3876788 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature