Structural basis for constitutive activity and agonist‐induced activation of the enteroendocrine fat sensor GPR119

GPR119 is a Gαs‐coupled 7TM receptor activated by endogenous lipids such as oleoylethanolamide (OEA) and by the dietary triglyceride metabolite 2‐monoacylglycerol. GPR119 stimulates enteroendocrine hormone and insulin secretion. But despite massive drug discovery efforts in the field, very little is known about the basic molecular pharmacology of GPR119.

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