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3PPM

Crystal Structure of a Noncovalently Bound alpha-Ketoheterocycle Inhibitor (Phenhexyl/Oxadiazole/Pyridine) to a Humanized Variant of Fatty Acid Amide Hydrolase

Summary for 3PPM
Entry DOI10.2210/pdb3ppm/pdb
Related2wj1 2wj2 3K7F 3K83 3K84 3PR0
DescriptorFatty-acid amide hydrolase 1, 7-phenyl-1-[5-(pyridin-2-yl)-1,3,4-oxadiazol-2-yl]heptan-1-one, CHLORIDE ION, ... (7 entities in total)
Functional Keywordsprotein-inhibitor complex, faah, oxazole, oxadiazole, endocannabinoid degradation, membrane protein, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
Biological sourceRattus norvegicus (rat)
Cellular locationEndoplasmic reticulum membrane; Single-pass membrane protein: P97612
Total number of polymer chains2
Total formula weight127649.30
Authors
Mileni, M.,Han, G.W.,Boger, D.L.,Stevens, R.C. (deposition date: 2010-11-24, release date: 2011-11-09, Last modification date: 2023-09-06)
Primary citationMileni, M.,Garfunkle, J.,Ezzili, C.,Cravatt, B.F.,Stevens, R.C.,Boger, D.L.
Fluoride-mediated capture of a noncovalent bound state of a reversible covalent enzyme inhibitor: X-ray crystallographic analysis of an exceptionally potent alpha-ketoheterocycle inhibitor of fatty acid amide hydrolase.
J.Am.Chem.Soc., 133:4092-4100, 2011
Cited by
PubMed: 21355555
DOI: 10.1021/ja110877y
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.78 Å)
Structure validation

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