3oj8

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Template:STRUCTURE 3oj8

Contents

Alpha-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Containing Additional Conformational Contraints in the Acyl Side Chain

Template:ABSTRACT PUBMED 21428410

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).

About this Structure

3oj8 is a 2 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

  • Ezzili C, Mileni M, McGlinchey N, Long JZ, Kinsey SG, Hochstatter DG, Stevens RC, Lichtman AH, Cravatt BF, Bilsky EJ, Boger DL. Reversible competitive alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. J Med Chem. 2011 Apr 28;54(8):2805-22. Epub 2011 Mar 23. PMID:21428410 doi:10.1021/jm101597x

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