Article
Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling.
European journal of medicinal chemistry - 15 Feb 2017
Plisson Fabien, Hill Timothy A, Mitchell Justin M, Hoang Huy N, de Araujo Aline D, Xu Weijun, Cotterell Adam, Edmonds David J, Stanton Robert V, Derksen David R, Loria Paula M, Griffith David A, Price David A, Liras Spiros, Fairlie David P
Abstract excerpt
Glucagon-like peptide (GLP-1) is an endogenous hormone that induces insulin secretion from pancreatic islets and modified forms are used to treat diabetes mellitus type 2. Understanding how GLP-1 interacts with its receptor (GLP-1R) can potentially lead to more effective drugs. Modeling and NMR studies of the N-terminus of GLP-1 suggest a β-turn between residues Glu9-Phe12 and a kinked alpha helix between...
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