52914-44-0Relevant academic research and scientific papers
NOVEL LIPASE INHIBITORS, REPORTER SUBSTRATES AND USES THEREOF
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Paragraph 0143, (2014/01/07)
The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment o f disorders comprising administration o f novel diacylglycerol lipase inhibitors, and com -positions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods o f assaying enzymatic activity com -prising contacting a compound with a novel ether lipid reporter compound.
Assay and inhibition of diacylglycerol lipase activity
Johnston, Meghan,Bhatt, Shachi R.,Sikka, Surina,Mercier, Richard W.,West, Jay M.,Makriyannis, Alexandros,Gatley, S. John,Duclos Jr., Richard I.
body text, p. 4585 - 4592 (2012/08/08)
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 standardized thin layer chromatography (TLC) radioassay of diacylglycerol lipase activity utilizing the labeled endogenous substrate [1″- 14C]1-stearoyl-2-arachidonoyl-sn-glycerol with phosphorimaging detection was used to quantify inhibition by following formation of the initial product [1″-14C]2-arachidonoylglycerol and further hydrolysis under the assay conditions to [1-14C]arachidonic acid.
