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Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)

Biochemistry. 2018-12; 
Pabst B, Futatsugi K, Li Q, Ahn K.
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Bacterial Expression System For the FLAG -tagged DGAT2 constructs, the cDNAs for DGAT2 were custom-synthesized at Genscript (Piscataway, NJ) and cloned into the pFastBac1 vector to generate an N-terminally FLAG-tagged pFastBac1-FLAG-DGAT2 (amino acids 1-388) construct. Get A Quote

摘要

Diacylglycerol acyltransferase 2 (DGAT2) catalyzes the final step in triacylglycerol (TAG) synthesis. Genetic knockdown or pharmacological inhibition of DGAT2 leads to a decrease in very-low-density lipoprotein TAG secretion and hepatic lipid levels in rodents, indicating DGAT2 may represent an attractive therapeutic target for treatment of hyperlipidemia and hepatic steatosis. We have previously described potent and selective imidazopyridine DGAT2 inhibitors with high oral bioavailability. However, the detailed mechanism of DGAT2 inhibition has not been reported. Herein, we describe imidazopyridines represented by PF-06424439 (1) and 2 as long residence time inhibitors of DGAT2. We demonstrate that 1 and 2 are... More

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