Targeting GLP-1 receptor trafficking to improve agonist efficacy.
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ABSTRACT:
SUBMITTER: Jones B
PROVIDER: S-EPMC5913239 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Publications
Targeting GLP-1 receptor trafficking to improve agonist efficacy.
Jones Ben B Buenaventura Teresa T Kanda Nisha N Chabosseau Pauline P Owen Bryn M BM Scott Rebecca R Goldin Robert R Angkathunyakul Napat N Corrêa Ivan R IR Bosco Domenico D Johnson Paul R PR Piemonti Lorenzo L Marchetti Piero P Shapiro A M James AMJ Cochran Blake J BJ Hanyaloglu Aylin C AC Inoue Asuka A Tan Tricia T Rutter Guy A GA Tomas Alejandra A Bloom Stephen R SR
Nature communications 20180423 1
Glucagon-like peptide-1 receptor (GLP-1R) activation promotes insulin secretion from pancreatic beta cells, causes weight loss, and is an important pharmacological target in type 2 diabetes (T2D). Like other G protein-coupled receptors, the GLP-1R undergoes agonist-mediated endocytosis, but the functional and therapeutic consequences of modulating GLP-1R endocytic trafficking have not been clearly defined. Here, we investigate a series of biased GLP-1R agonists with variable propensities for GLP ...[more]
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