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Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2015 Dec 10; Vol. 58 (23), pp. 9345-53. Date of Electronic Publication: 2015 Nov 20. - Publication Year :
- 2015
-
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.
- Subjects :
- Animals
Diacylglycerol O-Acyltransferase metabolism
Drug Discovery
Enzyme Inhibitors administration & dosage
Enzyme Inhibitors pharmacokinetics
Humans
Isoquinolines administration & dosage
Isoquinolines pharmacokinetics
Male
Mice
Mice, Inbred C57BL
Triglycerides blood
Diacylglycerol O-Acyltransferase antagonists & inhibitors
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Isoquinolines chemistry
Isoquinolines pharmacology
Triglycerides metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 58
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26561979
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.5b01345