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2005
Enzyme inhibiting activity
X 0220
Discovery of an Exceptionally Potent and Selective Class of Fatty Acid Amide HyInhibitors Enlisting Proteome-Wide Selectivity Screening: Concurrent
29- 221 drolase
Optimization of Enzyme Inhibitor Potency and Selectivity. — The concurrent implementation of a proteome-wide serine hydrolase selectivity screen with traditional efforts to optimize fatty acid amide hydrolase inhibition potency leads to the expedited
discovery of a new class of exceptionally potent and unusually selective inhibitors (I)
with a 1,3,4-oxadiazole skeleton. The synthesis is outlined and the screening procedure
is described. — (LEUNG, D.; DU, W.; HARDOUIN, C.; CHENG, H.; HWANG, I.;
CRAVATT, B. F.; BOGER*, D. L.; Bioorg. Med. Chem. Lett. 15 (2005) 5, 1423-1428;
Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037, USA; Eng.) —
H. Haber
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