Sandbox1111: Difference between revisions
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==Protein== | ==Protein== | ||
CYP2C8 is one of the principal hepatic drug-metabolizing enzymes that oxidizes therapeutic drugs such as taxol and cerivastatin and endobiotics such as retinoic acid and arachidonic acid. This protein has relatively large active site volume [go to Structure section and choose the green link to portray the active sites]. CYP2C8 crystallized as a symmetric dimer and is observed in solution. Furthermore, mass spectrometry confirmed the association of palmitic acid with the enzyme. This novel finding identifies a peripheral binding site in P450s that may contribute to drug-drug interactions in P450 metabolism. Perhaps an implement of Kerpolla's ingenious BiFC could provide a better understanding and monitoring of these drug-drug interactions. | |||
==Structure== | ==Structure== | ||
Revision as of 06:59, 22 May 2009
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Crystal Structure of Human Drug Metabolizing Cytochrome P450 2C8Crystal Structure of Human Drug Metabolizing Cytochrome P450 2C8
By Amit Shavit, 5/21/09
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| 3cin, resolution 1.70Å () | |||||||||
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| Ligands: | , , | ||||||||
| Gene: | TM1419, TM_1419 (Thermotoga maritima MSB8) | ||||||||
| Activity: | Inositol-3-phosphate synthase, with EC number 5.5.1.4 | ||||||||
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| Resources: | FirstGlance, OCA, RCSB, PDBsum, TOPSAN | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
ProteinProtein
CYP2C8 is one of the principal hepatic drug-metabolizing enzymes that oxidizes therapeutic drugs such as taxol and cerivastatin and endobiotics such as retinoic acid and arachidonic acid. This protein has relatively large active site volume [go to Structure section and choose the green link to portray the active sites]. CYP2C8 crystallized as a symmetric dimer and is observed in solution. Furthermore, mass spectrometry confirmed the association of palmitic acid with the enzyme. This novel finding identifies a peripheral binding site in P450s that may contribute to drug-drug interactions in P450 metabolism. Perhaps an implement of Kerpolla's ingenious BiFC could provide a better understanding and monitoring of these drug-drug interactions.
StructureStructure
are portrayed in purple.
are portrayed in blue
in red
in dark green
are shown in brown
ReferenceReference
Schoch GA, Yano JK, Wester MR, Griffin KJ, Stout CD, Johnson EF Structure of human microsomal cytochrome P450 2C8. Evidence for a peripheral fatty acid binding site. J Biol Chem. 2004 Mar 5;279(10):9497-503. Epub 2003 Dec 15. PMID:14676196