Fatty acid amide hydrolase

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This page, as it appeared on May 3, 2014, was featured in this article in the journal Biochemistry and Molecular Biology Education.

Fatty Acid Amide Hydrolase 1 (PDB: 2vya)

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  1. 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 1.8 Bracey MH, Hanson MA, Masuda KR, Stevens RC, Cravatt BF. Structural adaptations in a membrane enzyme that terminates endocannabinoid signaling. Science. 2002 Nov 29;298(5599):1793-6. PMID:12459591 doi:10.1126/science.1076535
  2. 2.0 2.1 2.2 2.3 Ahn K, Johnson DS, Mileni M, Beidler D, Long JZ, McKinney MK, Weerapana E, Sadagopan N, Liimatta M, Smith SE, Lazerwith S, Stiff C, Kamtekar S, Bhattacharya K, Zhang Y, Swaney S, Van Becelaere K, Stevens RC, Cravatt BF. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009 Apr 24;16(4):411-20. PMID:19389627 doi:10.1016/j.chembiol.2009.02.013
  3. 3.0 3.1 3.2 3.3 Mileni M, Johnson DS, Wang Z, Everdeen DS, Liimatta M, Pabst B, Bhattacharya K, Nugent RA, Kamtekar S, Cravatt BF, Ahn K, Stevens RC. Structure-guided inhibitor design for human FAAH by interspecies active site conversion. Proc Natl Acad Sci U S A. 2008 Sep 2;105(35):12820-4. Epub 2008 Aug 27. PMID:18753625
  4. Mileni M, Garfunkle J, DeMartino JK, Cravatt BF, Boger DL, Stevens RC. Binding and inactivation mechanism of a humanized fatty acid amide hydrolase by alpha-ketoheterocycle inhibitors revealed from cocrystal structures. J Am Chem Soc. 2009 Aug 5;131(30):10497-506. PMID:19722626 doi:10.1021/ja902694n
  5. 5.0 5.1 5.2 Mileni M, Kamtekar S, Wood DC, Benson TE, Cravatt BF, Stevens RC. Crystal structure of fatty acid amide hydrolase bound to the carbamate inhibitor URB597: discovery of a deacylating water molecule and insight into enzyme inactivation. J Mol Biol. 2010 Jul 23;400(4):743-54. Epub 2010 May 21. PMID:20493882 doi:10.1016/j.jmb.2010.05.034

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