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TitleBinding and Inactivation Mechanism of a Humanized Fatty Acid Amide Hydrolase by Alpha-Ketoheterocycle Inhibitors Revealed from Cocrystal Structures.
Journal, issue, pagesJ. Am. Chem. Soc., Vol. 131, Page 10497-, Year 2009
Publish dateMay 19, 2009 (structure data deposition date)
AuthorsMileni, M. / Garfunkle, J. / Demartino, J.K. / Cravatt, B.F. / Boger, D.L. / Stevens, R.C.
External linksJ. Am. Chem. Soc. / PubMed:19722626
MethodsX-ray diffraction
Resolution1.84 - 2.55 Å
Structure data

PDB-2wj1:
3D-crystal structure of humanized-rat fatty acid amide hydrolase (FAAH) conjugated with 7-phenyl-1-(4-(pyridin-2-yl)oxazol-2-yl)heptan- 1-one, an alpha-ketooxazole
Method: X-RAY DIFFRACTION / Resolution: 1.84 Å

PDB-2wj2:
3D-crystal structure of humanized-rat fatty acid amide hydrolase (FAAH) conjugated with 7-phenyl-1-(5-(pyridin-2-yl)oxazol-2-yl)heptan- 1-one, an alpha-ketooxazole
Method: X-RAY DIFFRACTION / Resolution: 2.55 Å

Chemicals

ChemComp-S99:
7-phenyl-1-(4-pyridin-2-yl-1,3-oxazol-2-yl)heptane-1,1-diol

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-OL1:
7-phenyl-1-(5-pyridin-2-yl-1,3-oxazol-2-yl)heptane-1,1-diol

Source
  • rattus norvegicus (Norway rat)
KeywordsHYDROLASE / MONOTOPIC MEMBRANE PROTEIN / FATTY ACID AMIDE HYDROLASE / GOLGI APPARATUS / ENDOPLASMIC RETICULUM / MEMBRANE / TRANSMEMBRANE / PHOSPHOPROTEIN / COVALENT REVERSIBLE INHIBITOR / COVALENT REVERSIBLE INHIBITORS / ALPHA-KETOOXAZOLE

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