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A novel low systemic diacylglycerol acyltransferase 1 inhibitor, Yhhu2407, improves lipid metabolism by Jun-Shang Huang; Bin-Bin Guo; Fei-Fei Lin; Li-Min Zeng; Ting Wang; Xiang-Yu Dang; Yang Yang; You-Hong Hu; Jia Liu; He-Yao Wang is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
What is A novel low systemic diacylglycerol acyltransferase 1 inhibitor, Yhhu2407, improves lipid metabolism about?
Diacylglycerol acyltransferase 1 (DGAT1) plays a pivotal role in lipid metabolism by catalyzing the committed step in triglyceride (TG) synthesis and has been considered as a potential therapeutic target of multiple metabolic diseases, including dyslipidemia, obesity and type 2 diabetes. Here we report a novel DGAT1 inhibitor, Yhhu2407, which showed a stronger DGAT1 inhibitory activity (IC = 18.24 ± 4.72 nM) than LCQ908 (IC = 78.24 ± 8.16 nM) in an enzymatic assay and led to a significant reduction in plasma TG after an acute lipid challenge in mice. Pharmacokinetic studies illustrated that Yhhu2407 displayed a low systemic, liver- and intestine-targeted distribution pattern, which is consistent with the preferential tissue expression pattern of DGAT1 and therefore might help to maximize the beneficial pharmacological effects and prevent the occurrence of side effects. Cell-based investigations demonstrated that Yhhu2407 inhibited free fatty acid (FFA)-induced TG accumulation and apolipoprotein B (ApoB)-100 secretion in HepG2 cells. In vivo study also disclosed that Yhhu2407 exerted a beneficial effect on regulating plasma TG and lipoprotein levels in rats, and effectively ameliora
Who reads A novel low systemic diacylglycerol acyltransferase 1 inhibitor, Yhhu2407, improves lipid metabolism?
It is typically read by researchers, students, and practitioners in Pharmacology, Toxicology and Pharmaceutics.
- Author
- Jun-Shang Huang; Bin-Bin Guo; Fei-Fei Lin; Li-Min Zeng; Ting Wang; Xiang-Yu Dang; Yang Yang; You-Hong Hu; Jia Liu; He-Yao Wang
- Publisher
- Elsevier BV
- Published
- 2020
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)