Reagents and models for detecting endogenous GLP1R and GIPR
Open accessAbstract
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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More recent studies using a variety of robust methodologies have concluded that there is no expression of GLP-1 receptor in human hepatocytes.
“more recent studies using a variety of robust methodologies have concluded that there is no expression in human hepatocytes.34”
From Randomised trial comparing weight loss through lifestyle and GLP-1 receptor agonist therapy in people with MASLD (2025) · cites this paper as [34]
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Structural and compositional diversity in the kainate receptor family
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Development and characterisation of a novel glucagon like peptide-1 receptor antibody
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Podewin, T., Ast, J., Broichhagen, J., Fine, N. H. F., Nasteska, D., Leippe, P., Gailer, M., Buenaventura, T., Kanda, N., Jones, B. J., et al. (2018) · ACS Central Science · doi:10.1021/acscentsci.7b00237 · Cited by 29 · see citing works
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Optoacoustic Imaging of Glucagon-like Peptide-1 Receptor with a Near-Infrared Exendin-4 Analog
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Sulfonated rhodamines as impermeable labelling substrates for cell surface protein visualizationPreprint
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Self-citationAn expanded LUXendin color palette for GLP1R detection and visualization in vitro and in vivoPreprint
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Self-citation
Flagged first, then by citations
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Drucker, D. J., & Holst, J. J. (2023) · Diabetologia · doi:10.1007/s00125-023-05906-7 · Cited by 243 · see citing works
GLP1R and GIPR expression and signaling in pancreatic alpha cells, beta cells and delta cells
Shilleh, A. H., Viloria, K., Broichhagen, J., Campbell, J. E., & Hodson, D. J. (2024) · Peptides · doi:10.1016/j.peptides.2024.171179 · Cited by 39 · see citing works
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Glucose-dependent insulinotropic polypeptide receptor signaling alleviates gut inflammation in mice
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Reassessment of antibody-based detection of the murine T cell GLP-1 receptor
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Self-citation
- 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)
- PMC
- PMC8669301
- 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
- gold
- doi.org
- Licence
- 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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