Ontology highlight
ABSTRACT:
SUBMITTER: Serrano-Wu MH
PROVIDER: S-EPMC4025815 | biostudies-other | 2012 May
REPOSITORIES: biostudies-other
ACS medicinal chemistry letters 20120404 5
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 un ...[more]