GPR40: A therapeutic target for mediating insulin secretion
Open accessAbstract
G-protein-coupled receptor 40 (GPR40), known as free fatty acid receptor 1, is mainly expressed in pancreatic β-cells and activated by medium- and long-chain fatty acids. Increasing evidence indicates that the activation of GPR40 in cells causes insulin secretion, and GPR40 has become an attractive therapeutic target for type 2 diabetes. Recently, certain novel GPR40 agonists have been identified that regulate glucose-stimulated insulin secretion, leading to the development of new drugs for the treatment of type 2 diabetes. In this review, we focus on progress in the physiological role of GPR40 and potential drugs targeting GPR40 over the past decade.
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PFOS can stimulate insulin secretion and intracellular calcium level by activating G protein-coupled receptor 40 (GPR40).
“A recent study showed that PFOS can stimulate insulin”
From Exposure to per- and polyfluoroalkyl substances in early pregnancy, risk of gestational diabetes mellitus, potential pathways, and influencing factors in pregnant women: A nested case-control study (2023) · cites this paper as Feng et al., 2012
Section 4, “Physiological role of GPR40 in mediating insulin secretion” (page not available), describes GPR40 activation increasing cytoplasmic calcium and promoting insulin secretion. It discusses fatty acids and other agonists, but does not identify PFOS as an agonist or report that PFOS produces these effects. (LLM, conf=0.85)
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Thiazolidinediones and Heart Failure
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Role of GPR40 in fatty acid action on the β cell line INS-1E
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Zang, L., Liu, X., Xie, X., Zhou, X., Pan, Y., & Dai, J. (2023) · Environmental Pollution · doi:10.1016/j.envpol.2023.121504 · Cited by 42 · see citing works
Multitarget PPARγ Agonists as Innovative Modulators of the Metabolic Syndrome
Ammazzalorso, A., Maccallini, C., Amoia, P., & Amoroso, R. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.04.030 · Cited by 39 · see citing works
- Authors
- FENG, X.-T., LENG, J., XIE, Z., LI, S.-L., ZHAO, W., & TANG, Q.-L.
- Affiliations
- Guangxi University of Chinese Medicine (CN)
- The First Affiliated Hospital of Guangxi University of Traditional Chinese Medicine (CN)
- ORCID
- Venue
- International Journal of Molecular Medicine
- Publisher
- Spandidos Publications
- Published
- 2012-09-26
- Volume
- 30
- Issue
- 6
- Pages
- 1261-1266
- ISSN
- 1107-3756 (ISSN-L)
- 1791-244X
- OpenAlex
- W1996947378
- Cited by
- 54
- References
- 4
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 4 · 2023: 3 · 2022: 2 · 2021: 4 · 2020: 5 · 2019: 5 · 2018: 2 · 2017: 6 · 2016: 7 · 2015: 4 · 2014: 7 · 2013: 1
- FWCI
- 0.74
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- International Journal of Molecular Medicine (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (81202677)
- Natural Science Foundation of Guangxi Province
- Topics
- Health Sciences › Medicine › Surgery › Pancreatic function and diabetes
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- GPR40, free fatty acid receptor 1, insulin secretion, pancreatic beta cells, type 2 diabetes, GPR40 agonist, glucose-stimulated insulin secretion, fatty acid signaling, therapeutic target
- MeSH terms
- Insulin Secretion, Animals, Benzofurans, Berberine, Diabetes Mellitus, Type 2, Fatty Acids, Nonesterified, Humans, Hypoglycemic Agents, Insulin, Ligands, Sulfones, Clinical Trials, Phase II as Topic, Receptors, G-Protein-Coupled, Molecular Targeted Therapy
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