3qk5 | pdb_00003qk5

Crystal structure of fatty acid amide hydrolase with small molecule inhibitor

spinqualitylabelsall models 3qk5, resolution 2.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3qk5 is a 2 chain structure with sequence from Buffalo rat. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: EDO, GOL, QK5 Related: 3qj8, 3qj9, 3qkv Gene: Faah, Faah1 (Buffalo rat) Activity: Fatty acid amide hydrolase, with EC number 3.5.1.99 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [FAAH1_RAT] Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules. Hydrolyzes polyunsaturated substrate anandamide preferentially as compared to monounsaturated substrates (By similarity). Publication Abstract from PubMed Starting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and synthesized. These efforts identified a series of novel, noncovalent FAAH inhibitors with in vitro potency comparable to known covalent FAAH inhibitors. The mechanism of action for these compounds was determined through a combination of SAR and co-crystallography with rat FAAH. Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.,Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F Bioorg Med Chem Lett. 2011 Apr 15;21(8):2492-6. Epub 2011 Feb 17. PMID:21392988 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Fatty acid amide hydrolase

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