The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules
Open accessAbstract
Long chain fatty acids have recently been identified as agonists for the G protein‐coupled receptors GPR40 and GPR120. Here, we present the first description of GW9508, a small‐molecule agonist of the fatty acid receptors GPR40 and GPR120. In addition, we also describe the pharmacology of GW1100, a selective GPR40 antagonist. These molecules were used to further investigate the role of GPR40 in glucose‐stimulated insulin secretion in the MIN6 mouse pancreatic β‐cell line. GW9508 and linoleic acid both stimulated intracellular Ca 2+ mobilization in human embryonic kidney (HEK)293 cells expressing GPR40 (pEC 50 values of 7.32±0.03 and 5.65±0.06, respectively) or GPR120 (pEC 50 values of 5.46±0.09 and 5.89±0.04, respectively), but not in the parent HEK‐293 cell line. GW1100 dose dependently inhibited GPR40‐mediated Ca 2+ elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW1100 had no effect on the GPR120‐mediated stimulation of intracellular Ca 2+ release produced by either GW9508 or linoleic acid. GW9508 dose dependently potentiated glucose‐stimulated insulin secretion in MIN6 cells, but not in primary rat or mouse islets. Furthermore, GW9508 was able to potentiate the KCl‐mediated increase in insulin secretion in MIN6 cells. The effects of GW9508 on insulin secretion were reversed by GW1100, while linoleic acid‐stimulated insulin secretion was partially attenuated by GW1100. These results add further evidence to a link between GPR40 and the ability of fatty acids to acutely potentiate insulin secretion and demonstrate that small‐molecule GPR40 agonists are glucose‐sensitive insulin secretagogues. British Journal of Pharmacology (2006) 148, 619–628. doi:10.1038/sj.bjp.0706770
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Brown, A. J., Goldsworthy, S. M., Barnes, A. A., Eilert, M. M., Tcheang, L., Daniels, D., Muir, A. I., Wigglesworth, M. J., Kinghorn, I., Fraser, N. J., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m211609200 · Cited by 2,409
Self-citationLe Poul, E., Loison, C., Struyf, S., Springael, J.-Y., Lannoy, V., Decobecq, M.-E., Brezillon, S., Dupriez, V., Vassart, G., Van Damme, J., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m301403200 · Cited by 1,651
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
Itoh, Y., Kawamata, Y., Harada, M., Kobayashi, M., Fujii, R., Fukusumi, S., Ogi, K., Hosoya, M., Tanaka, Y., Uejima, H., et al. (2003) · Nature · doi:10.1038/nature01478 · Cited by 1,538
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Role of GPR40 in fatty acid action on the β cell line INS-1E
Shapiro, H., Shachar, S., Sekler, I., Hershfinkel, M., & Walker, M. D. (2005) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2005.07.042 · Cited by 220 · cited 4×
“…an increase in [Ca2þ ]i and insulin secretion, mediated via activation of phospholipase C (PLC) resulting in the release of calcium from the endoplasmic reticulum and upregulation of calcium influx via L-type calcium channels preactivated by glucose ((Fujiwara et al., 2005; Shapiro et al., 2005).”
BackgroundResultInfluentialOlofsson, C. S., Salehi, A., Holm, C., & Rorsman, P. (2004) · The Journal of Physiology · doi:10.1113/jphysiol.2004.066258 · Cited by 88
Cited by
Oh, D. Y., Talukdar, S., Bae, E. J., Imamura, T., Morinaga, H., Fan, W., Li, P., Lu, W. J., Watkins, S. M., & Olefsky, J. M. (2010) · Cell · doi:10.1016/j.cell.2010.07.041 · Cited by 2,428
“However, this compound was not specific and also stimulated GPR120 (Briscoe et al., 2006).”
Free Fatty Acid Receptors in Health and Disease
Kimura, I., Ichimura, A., Ohue-Kitano, R., & Igarashi, M. (2020) · Physiological Reviews · doi:10.1152/physrev.00041.2018 · Cited by 1,018
Yan, Y., Jiang, W., Spinetti, T., Tardivel, A., Castillo, R., Bourquin, C., Guarda, G., Tian, Z., Tschopp, J., & Zhou, R. (2013) · Immunity · doi:10.1016/j.immuni.2013.05.015 · Cited by 784
G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. M., & Langmead, C. J. (2018) · Pharmacological Reviews · doi:10.1124/pr.117.014373 · Cited by 108
Yashiro, H., Tsujihata, Y., Takeuchi, K., Hazama, M., Johnson, P. R. V., & Rorsman, P. (2012) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.187708 · Cited by 84
Metadata
- Authors
- Briscoe, C. P., Peat, A. J., McKeown, S. C., Corbett, D. F., Goetz, A. S., Littleton, T. R., McCoy, D. C., Kenakin, T. P., Andrews, J. L., Ammala, C., Fornwald, J. A., Ignar, D. M., & Jenkinson, S.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2006-07
- Volume
- 148
- Issue
- 5
- Pages
- 619-628
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2089540591
- Cited by
- 400
- References
- 6
- FWCI
- 16.83
- Type
- journal article
- Language
- en
- Open access
- bronze
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- The paper
- Briscoe, C. P., Peat, A. J., McKeown, S. C., Corbett, D. F., Goetz, A. S., Littleton, T. R., McCoy, D. C., Kenakin, T. P., Andrews, J. L., Ammala, C., Fornwald, J. A., Ignar, D. M., & Jenkinson, S. (2006). Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. British Journal of Pharmacology. https://doi.org/10.1038/sj.bjp.0706770
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