Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery.

ABSTRACT: The glucagon-like peptide-1 receptor (GLP-1R) controls the physiological responses to the incretin hormone glucagon-like peptide-1 and is a major therapeutic target for the treatment of type 2 diabetes, owing to the broad range of effects that are mediated upon its activation. These include the promotion of glucose-dependent insulin secretion, increased insulin biosynthesis, preservation of β-cell mass, improved peripheral insulin action, and promotion of weight loss. Regulation of GLP-1R function is complex, with multiple endogenous and exogenous peptides that interact with the receptor that result in the activation of numerous downstream signaling cascades. The current understanding of GLP-1R signaling and regulation is limited, with the desired spectrum of signaling required for the ide

SUBMITTER: Koole C 

PROVIDER: S-EPMC3725346 | biostudies-literature | 2013 Aug

REPOSITORIES: biostudies-literature