DGAT1 inhibitors as anti-obesity and anti-diabetic agents.
Explore this paper's citation graph
Summary
Since 2008, significant advances have been made in understanding the role of diacylglycerol acyl transferase-1 in disease states such as diabetes and obesity, which has resulted in a new generation of DGAT1 inhibitors that have progressed into clinical development, with the leading compound LCQ-908 now in phase II clinical trials.
- Type
- article
- Published
- 2010-07-01
- Cited by
- 83
- References
- 0
- OpenAlex
- https://openalex.org/W175847418
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:24576217
Keywords
Diabetes mellitus, Obesity, Anti obesity, Clinical trial, Pharmacology
References
No references recorded for this paper.
Cited by
- Gene silencing approaches for the management of dyslipidaemia.
- Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
- Type 2 diabetes mellitus
- Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes.
- Identification of a botanical inhibitor of intestinal diacylglyceride acyltransferase 1 activity via in vitro screening and a parallel, randomized, blinded, placebo-controlled clinical trial
- Membrane-bound O-acyltransferases (MBOATs)
- Pharmacological inhibition of diacylglycerol acyltransferase 1 reduces body weight and modulates gut peptide release—Potential insight into mechanism of action
- DGAT1 mutation is linked to a congenital diarrheal disorder.
- Regulating intestinal function to reduce atherogenic lipoproteins
- Preclinical pharmacokinetic characterization of 2-(4-(4-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)-1H-benzo[d]imidazol-2-yl)phenyl)cyclohexyl) acetic acid, a novel DGAT-1 inhibitor
- Intestine-specific Deletion of Acyl-CoA:Monoacylglycerol Acyltransferase (MGAT) 2 Protects Mice from Diet-induced Obesity and Glucose Intolerance*
- Acyl-CoA:Diacylglycerol Acyltransferase: A Key Player in the Regulation of Fatty Acid and Glucose Metabolism in Mammalian Systems
- Prise en charge des hypertriglycéridémies sévères
- Treating Hepatitis C Infection by Targeting the Host
- Investigation of the conformational flexibility of DGAT1 peptides using tryptophan fluorescence
- Diacylglycerol acyltransferase 1 inhibition with AZD7687 alters lipid handling and hormone secretion in the gut with intolerable side effects: a randomized clinical trial
- Direct-acting and host-targeting HCV inhibitors: current and future directions.
- Cardiomyocyte-specific Loss of Diacylglycerol Acyltransferase 1 (DGAT1) Reproduces the Abnormalities in Lipids Found in Severe Heart Failure*
- Peritumoral Expression of Adipokines and Fatty Acids in Breast Cancer
- Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
Related papers
- Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking Dgat
- Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis.
- DGAT enzymes and triacylglycerol biosynthesis
- Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
- Cloning of DGAT2, a Second Mammalian Diacylglycerol Acyltransferase, and Related Family Members*
- Inhibition of Triglyceride Synthesis as a Treatment Strategy for Obesity
- Targeting Acyl-CoA:Diacylglycerol Acyltransferase 1 (DGAT1) with Small Molecule Inhibitors for the Treatment of Metabolic Diseases
- Increased insulin and leptin sensitivity in mice lacking acyl CoA:diacylglycerol acyltransferase 1.
- DGAT1 Is Not Essential for Intestinal Triacylglycerol Absorption or Chylomicron Synthesis*
- Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.