{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["3(5)"],"submitter":["Serrano-Wu MH"],"pubmed_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."],"journal":["ACS medicinal chemistry letters"],"pagination":["411-5"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4025815"],"repository":["biostudies-literature"],"pubmed_title":["Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides."],"pmcid":["PMC4025815"],"pubmed_authors":["Neubert AD","Coppola GM","Yoon T","Jain M","Chatelain R","Serrano-Wu MH","Mullarkey T","Commerford R","Sung MJ","Gong Y","Hou Y","Li L","Tyler A","Daniels T","Cosker T","Clairmont KB","Yang Q","Rocheford E","Hubbard BK","Juedes M"],"additional_accession":[]},"is_claimable":false,"name":"Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.","description":"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.","dates":{"release":"2012-01-01T00:00:00Z","publication":"2012 May","modification":"2025-04-04T08:41:47.321Z","creation":"2019-03-27T01:28:29Z"},"accession":"S-EPMC4025815","cross_references":{"pubmed":["24900485"],"doi":["10.1021/ml3000512"]}}