Cited by 40Diabetes Treatment and ManagementReceptor Mechanisms and SignalingRegulation of Appetite and Obesity

Reagents and models for detecting endogenous GLP1R and GIPR

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Ast, Julia, Broichhagen, Johannes, Hodson, David J.·2021·EBioMedicine

Abstract

Glucagon-like peptide-1 receptor (GLP1R) agonists target the GLP1R, whereas dual GLP1R/ gastric inhibitory polypeptide receptor (GIPR) agonists target both the GLP1R and GIPR. Despite the importance of these drug classes for the treatment of diabetes and obesity, still very little is known about the localization of GLP1R and GIPR themselves. Complicating matters is the low abundance of GLP1R and GIPR mRNA/protein, as well as a lack of specific and validated reagents for their detection. Without knowing where GLP1R and GIPR are located, it is difficult to propose mechanisms of action in the various target organs, and whether this is indirect or direct. In the current review, we will explain the steps needed to properly validate reagents for endogenous GLP1R/GIPR detection, describe the available approaches to visualize GLP1R/GIPR, and provide an update on the state-of-art. The overall aim is to provide a reference resource for researchers interested in GLP1R and GIPR signaling.

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  1. [96]Drucker DJ. Mechanisms of action and therapeutic application of Glucagon-like Peptide-1 Cell Metab 27 4 2018 740 756 29617641
  2. [97]Lehtonen J Schäffer L Rasch MG Hecksher-Sørensen J Ahnfelt-Rønne J. Beta cell specific probing with fluorescent exendin-4 is progressively reduced in type 2 diabetic mouse models Islets 7 6 2016 e1137415 PMC4878261 26963143

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Authors
Ast, J., Broichhagen, J., & Hodson, D. J.
Affiliations
  • University of Birmingham (GB)
  • Leibniz-Forschungsinstitut für Molekulare Pharmakologie (DE)
Corresponding author
  • Broichhagen, Johannes
  • Hodson, David J.
Venue
EBioMedicine
Publisher
Elsevier BV
Published
2021-12
Volume
74
Pages
103739
ISSN
2352-3964 (ISSN-L)
OpenAlex
W4200059665
Cited by
40
References
97
Citations by year
2026: 7 · 2025: 13 · 2024: 8 · 2023: 4 · 2022: 8
FWCI
0.77
Type
journal article
Language
en
Open access
Locations
  • EBioMedicine (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
  • Medical Research Council (MR/N00275X/1, MR/S025618/1)
  • Diabetes UK (17/0005681)
  • University of Cambridge
  • European Research Council
  • Horizon 2020
  • ERC (715884)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
Keywords
GLP-1 receptor, reagent validation, receptor localization, receptor visualization, diabetes mellitus, obesity
MeSH terms
Glucagon-Like Peptide-1 Receptor, Animals, Humans, Microscopy, Electron, Pancreas, Receptors, Gastrointestinal Hormone, Signal Transduction

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