Assay and inhibition of diacylglycerol lipase activity

…, S Sikka, RW Mercier, JM West, A Makriyannis…

Index: Johnston, Meghan; Bhatt, Shachi R.; Sikka, Surina; Mercier, Richard W.; West, Jay M.; Makriyannis, Alexandros; Gatley, S. John; Duclos Jr., Richard I. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4585 - 4592

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Citation Number: 9

Abstract

A series of N-formyl-α-amino acid esters of β-lactone derivatives structurally related to tetrahydrolipstatin (THL) and O-3841 were synthesized that inhibit human and murine diacylglycerol lipase (DAGL) activities. New ether lipid reporter compounds were developed for an in vitro assay to efficiently screen inhibitors of 1, 2-diacyl-sn-glycerol hydrolysis and related lipase activities using fluorescence resonance energy transfer (FRET). A ...