Agonist-induced membrane nanodomain clustering drives GLP-1 receptor responses in pancreatic beta cells.
File(s)journal.pbio.3000097.pdf (4.51 MB)
Published version
Author(s)
Type
Journal Article
Abstract
The glucagon-like peptide-1 receptor (GLP-1R), a key pharmacological target in type 2 diabetes (T2D) and obesity, undergoes rapid endocytosis after stimulation by endogenous and therapeutic agonists. We have previously highlighted the relevance of this process in fine-tuning GLP-1R responses in pancreatic beta cells to control insulin secretion. In the present study, we demonstrate an important role for the translocation of active GLP-1Rs into liquid-ordered plasma membrane nanodomains, which act as hotspots for optimal coordination of intracellular signaling and clathrin-mediated endocytosis. This process is dynamically regulated by agonist binding through palmitoylation of the GLP-1R at its carboxyl-terminal tail. Biased GLP-1R agonists and small molecule allosteric modulation both influence GLP-1R palmitoylation, clustering, nanodomain signaling, and internalization. Downstream effects on insulin secretion from pancreatic beta cells indicate that these processes are relevant to GLP-1R physiological actions and might be therapeutically targetable.
Date Issued
2019-08-20
Date Acceptance
2019-08-05
Citation
PLoS Biology, 2019, 17 (8), pp.1-40
ISSN
1544-9173
Publisher
Public Library of Science (PLoS)
Start Page
1
End Page
40
Journal / Book Title
PLoS Biology
Volume
17
Issue
8
Copyright Statement
© 2019 Buenaventura et al. This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Sponsor
Genesis Research Trust
Diabetes UK
Wellcome Trust
Medical Research Council (MRC)
Identifier
https://www.ncbi.nlm.nih.gov/pubmed/31430273
PII: PBIOLOGY-D-18-01320
Grant Number
1064
15/0005374
212625/Z/18/Z
MR/R010676/1
Subjects
Developmental Biology
06 Biological Sciences
11 Medical and Health Sciences
07 Agricultural and Veterinary Sciences
Publication Status
Published
Coverage Spatial
United States
Date Publish Online
2019-08-20