title: The first structure of a microsomal P450--implications for drug discovery.
abstract: Although numerous microbial, soluble P450 structures have been known for some time, it is only recently that the first crystal structure of a microsomal, membrane-associated P450 has been determined. The structure gives an increased understanding of the membrane, substrate and reductase binding surfaces, and has enabled the modeling of other P450s with greater accuracy. Other milestones include the first determination of a true P450 drug target, CYP51, the determination of a thermophilic P450 and the structures of cryogenically trapped intermediates of the P450 reaction cycle.
authors.affiliation: Syrrx Inc., 10450 Science Center Drive, Suite 100, San Diego, CA 92121, USA.
authors.forename: M
authors.initials: M
authors.lastname: Tennant
authors.forename: D E
authors.initials: DE
authors.lastname: McRee
mesh_terms: D000818:Animals; D002874:Chromosome Mapping; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000737:chemistry* / Q000235:genetics; D015195:Drug Design; D006801:Humans; D008861:Microsomes / Q000201:enzymology*; D008958:Models, Molecular; D011485:Protein Binding; D021281:Quantitative Structure-Activity Relationship
chemical_list: D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System