1e9x
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CYTOCHROME P450 14 ALPHA-STEROL DEMETHYLASE (CYP51) FROM MYCOBACTERIUM TUBERCULOSIS IN COMPLEX WITH 4-PHENYLIMIDAZOLE
OverviewOverview
Cytochrome P450 14alpha-sterol demethylases (CYP51) are essential enzymes, in sterol biosynthesis in eukaryotes. CYP51 removes the 14alpha-methyl, group from sterol precursors such as lanosterol, obtusifoliol, dihydrolanosterol, and 24(28)-methylene-24,25-dihydrolanosterol., Inhibitors of CYP51 include triazole antifungal agents fluconazole and, itraconazole, drugs used in treatment of topical and systemic mycoses. The, 2.1- and 2.2-A crystal structures reported here for 4-phenylimidazole- and, fluconazole-bound CYP51 from Mycobacterium tuberculosis (MTCYP51) are the, first structures of an authentic P450 drug target. MTCYP51 exhibits the, P450 fold with the exception of two striking differences-a bent I helix, and an open conformation of BC loop-that define an active site-access, channel ... [(full description)]
About this StructureAbout this Structure
1E9X is a [Single protein] structure of sequence from [Mycobacterium tuberculosis] with HEM and PIM as [ligands]. Structure known Active Sites: HEM and PIM. Full crystallographic information is available from [OCA].
ReferenceReference
Crystal structure of cytochrome P450 14alpha -sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with azole inhibitors., Podust LM, Poulos TL, Waterman MR, Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3068-73. PMID:11248033
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