1w0f: Difference between revisions
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==Overview== | ==Overview== | ||
Cytochromes P450 (P450s) metabolize a wide range of endogenous compounds, and xenobiotics, such as pollutants, environmental compounds, and drug, molecules. The microsomal, membrane-associated, P450 isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, and CYP1A2 are responsible for the, oxidative metabolism of more than 90% of marketed drugs. Cytochrome P450, 3A4 (CYP3A4) metabolizes more drug molecules than all other isoforms, combined. Here we report three crystal structures of CYP3A4: unliganded, bound to the inhibitor metyrapone, and bound to the substrate, progesterone. The structures revealed a surprisingly small active site, with little conformational change associated with the binding of either, compound. An unexpected peripheral binding site is identified, located, above a . | Cytochromes P450 (P450s) metabolize a wide range of endogenous compounds, and xenobiotics, such as pollutants, environmental compounds, and drug, molecules. The microsomal, membrane-associated, P450 isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, and CYP1A2 are responsible for the, oxidative metabolism of more than 90% of marketed drugs. Cytochrome P450, 3A4 (CYP3A4) metabolizes more drug molecules than all other isoforms, combined. Here we report three crystal structures of CYP3A4: unliganded, bound to the inhibitor metyrapone, and bound to the substrate, progesterone. The structures revealed a surprisingly small active site, with little conformational change associated with the binding of either, compound. An unexpected peripheral binding site is identified, located, above a phenylalanine cluster, which may be involved in the initial, recognition of substrates or allosteric effectors. | ||
==About this Structure== | ==About this Structure== | ||
1W0F is a | 1W0F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with HEM and STR as [http://en.wikipedia.org/wiki/ligands ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1W0F OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: oxidoreductase]] | [[Category: oxidoreductase]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:47:57 2007'' | ||
