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Updated: Apr 28, 2026

A Fluorescence-based Assay for Characterization and Quantification of Lipid Droplet Formation in Human Intestinal Organoids
Published on: October 13, 2019
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial
Michael H Serrano-Wu1, Gary M Coppola1, Yongjin Gong1
1Departments of Global Discovery Chemistry, Cardiovascular and Metabolism, Metabolism and Pharmacokinetics, and Translational Sciences, Novartis Institutes for Biomedical Research , 100 Technology Square, Cambridge Massachusetts 02139, United States.
Abstract:
High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut is an attractive drug discovery strategy with anticipated benefits of reduced systemic toxicity. In this report we describe our discovery and optimization of DGAT1 inhibitors whose plasma exposure is minimized by the action of transporters, including the P-glycoprotein transporter. The impact of this unique absorption profile on efficacy in rat and dog efficacy models is presented.
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