Abstract
DGAT2 plays a critical role in hepatic triglyceride production, and data suggests that inhibition of DGAT2 could prove to be beneficial in treating a number of disease states. This article documents the discovery and optimization of a selective small molecule inhibitor of DGAT2 as well as pharmacological proof of biology in a mouse model of triglyceride production.
MeSH terms
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Animals
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Diacylglycerol O-Acyltransferase / antagonists & inhibitors*
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Diacylglycerol O-Acyltransferase / metabolism
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Drug Discovery
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology*
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Humans
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Isoquinolines / administration & dosage
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Isoquinolines / chemistry*
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Isoquinolines / pharmacokinetics
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Isoquinolines / pharmacology*
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Male
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Mice
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Mice, Inbred C57BL
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Triglycerides / blood
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Triglycerides / metabolism*
Substances
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Enzyme Inhibitors
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Isoquinolines
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Triglycerides
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DGAT2 protein, human
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Diacylglycerol O-Acyltransferase