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TitleDeterminants of cytochrome P450 2C8 substrate binding: structures of complexes with montelukast, troglitazone, felodipine, and 9-cis-retinoic acid.
Journal, issue, pagesJ. Biol. Chem., Vol. 283, Page 17227-17237, Year 2008
Publish dateOct 24, 2006 (structure data deposition date)
AuthorsSchoch, G.A. / Yano, J.K. / Sansen, S. / Dansette, P.M. / Stout, C.D. / Johnson, E.F.
External linksJ. Biol. Chem. / PubMed:18413310
MethodsX-ray diffraction
Resolution2.28 - 2.8 Å
Structure data

PDB-2nnh:
CYP2C8dH complexed with 2 molecules of 9-cis retinoic acid
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

PDB-2nni:
CYP2C8dH complexed with montelukast
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

PDB-2nnj:
CYP2C8dH complexed with felodipine
Method: X-RAY DIFFRACTION / Resolution: 2.28 Å

PDB-2vn0:
CYP2C8DH COMPLEXED WITH TROGLITAZONE
Method: X-RAY DIFFRACTION / Resolution: 2.7 Å

Chemicals

ChemComp-SO4:
SULFATE ION

ChemComp-HEM:
PROTOPORPHYRIN IX CONTAINING FE

ChemComp-9CR:
(9cis)-retinoic acid / anticancer, antineoplastic*YM

ChemComp-PLM:
PALMITIC ACID

ChemComp-HOH:
WATER

ChemComp-MTK:
MONTELUKAST / medication*YM

ChemComp-225:
FELODIPINE / medication, channel blocker*YM

ChemComp-TDZ:
(5R)-5-(4-{[(2R)-6-HYDROXY-2,5,7,8-TETRAMETHYL-3,4-DIHYDRO-2H-CHROMEN-2-YL]METHOXY}BENZYL)-1,3-THIAZOLIDINE-2,4-DIONE / antiinflammatory*YM

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / ELECTRON TRANSPORT / CYP2C8; Human P450 2C8; monooxygenases; substrate complex; palmitic acid; 9-cis retinoic acid; panretin / CYP2C8; Human P450 2C8; monooxygenases; Montelukast; Singulair; inhibitor complex; palmitic aci / CYP2C8; Human P450 2C8; monooxygenases; Felodipine; Plendil; inhibitor complex; palmitic acid / ENDOPLASMIC RETICULUM / METAL-BINDING / PALMITIC ACID / HUMAN P450 2C8 / TROGLITAZONE / POLYMORPHISM / MONOOXYGENASE / IRON / HEME / CYP2C8 / MEMBRANE / MICROSOME / MONOOXYGENASES / INHIBITOR COMPLEX

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