GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

作者: Maria Hauge , Marie A. Vestmar , Anna S. Husted , Jeppe P. Ekberg , Michael J. Wright

DOI: 10.1016/J.MOLMET.2014.10.002

关键词:

摘要: Objectives GPR40 (FFAR1), a clinically proven anti-diabetes target, is Gq-coupled receptor for long chain fatty acids (LCFA) stimulating insulin secretion directly and mediating major part of the dietary triglyceride-induced incretins GLP-1 GIP. In phase-II studies GPR40 agonist TAK-875 decreased blood glucose but surprisingly without incretins.

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