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Cited by 1,104

The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.

The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids

Open access
Briscoe, Celia P., Tadayyon, Mohammad, Andrews, John L., Benson, William G., Chambers, Jon K., Eilert, Michelle M., Ellis, Catherine, Elshourbagy, Nabil A., Goetz, Aaron S., Minnick, Dana T., Murdock, Paul R., Sauls, Howard R., Shabon, Usman, Spinage, Lisa D., Strum, Jay C., Szekeres, Philip G., Tan, Kong B., Way, James M., Ignar, Diane M., Wilson, Shelagh, Muir, Alison I.·2003·Journal of Biological Chemistry

Abstract

GPR40 is a member of a subfamily of homologous G protein-coupled receptors that include GPR41 and GPR43 and that have no current function or ligand ascribed. Ligand fishing experiments in HEK293 cells expressing human GPR40 revealed that a range of saturated and unsaturated carboxylic acids with carbon chain lengths greater than six were able to induce an elevation of [Ca(2+)](i), measured using a fluorometric imaging plate reader. 5,8,11-Eicosatriynoic acid was the most potent fatty acid tested, with a pEC(50) of 5.7. G protein coupling of GPR40 was examined in Chinese hamster ovary cells expressing the G alpha(q/i)-responsive Gal4-Elk1 reporter system. Expression of human GPR40 led to a constitutive induction of luciferase activity, which was further increased by exposure of the cells to eicosatriynoic acid. Neither the constitutive nor ligand-mediated luciferase induction was inhibited by pertussis toxin treatment, suggesting that GPR40 was coupled to G alpha(q/11.) Expression analysis by quantitative reverse transcription-PCR showed that GPR40 was specifically expressed in brain and pancreas, with expression in rodent pancreas being localized to insulin-producing beta-cells. These data suggest that some of the physiological effects of fatty acids in pancreatic islets and brain may be mediated through a cell-surface receptor.

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Metadata

Authors
Briscoe, C. P., Tadayyon, M., Andrews, J. L., Benson, W. G., Chambers, J. K., Eilert, M. M., Ellis, C., Elshourbagy, N. A., Goetz, A. S., Minnick, D. T., Murdock, P. R., Sauls, H. R., Shabon, U., Spinage, L. D., Strum, J. C., Szekeres, P. G., Tan, K. B., Way, J. M., Ignar, D. M., Wilson, S., & Muir, A. I.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
2003-03
Volume
278
Issue
13
Pages
11303-11311
ISSN
0021-9258 (ISSN-L)
OpenAlex
W2102964449
Cited by
1,104
References
3
FWCI
9.01
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids. https://app.cochat.ai/papers/10.1074/jbc.m211495200
The paper
Briscoe, C. P., Tadayyon, M., Andrews, J. L., Benson, W. G., Chambers, J. K., Eilert, M. M., Ellis, C., Elshourbagy, N. A., Goetz, A. S., Minnick, D. T., Murdock, P. R., Sauls, H. R., Shabon, U., Spinage, L. D., Strum, J. C., Szekeres, P. G., Tan, K. B., Way, J. M., Ignar, D. M., . . . Muir, A. I. (2003). The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m211495200

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.