The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Discovery of a Potent and Selective GPR120 Agonist
Open accessAbstract
GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.
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Citations
Cites
Type 2 diabetes as an inflammatory disease
Donath, M. Y., & Shoelson, S. E. (2011) · Nature Reviews Immunology · doi:10.1038/nri2925 · Cited by 3,737
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
Unsaturated fatty acids revert diet-induced hypothalamic inflammation in obesity
Cintra, D. E., Ropelle, E. R., Moraes, J. C., Pauli, J. R., Morari, J., de Souza, C. T., Grimaldi, R., Stahl, M., Carvalheira, J. B., Saad, M. J., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0030571 · Cited by 381
Cited by
A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice
Oh, D. Y., Walenta, E., Akiyama, T. E., Lagakos, W. S., Lackey, D., Pessentheiner, A. R., Sasik, R., Hah, N., Chi, T. J., Cox, J. M., et al. (2014) · Nature Medicine · doi:10.1038/nm.3614 · Cited by 391
Auguste, S., Fisette, A., Fernandes, M. F., Hryhorczuk, C., Poitout, V., Alquier, T., & Fulton, S. (2016) · International Journal of Neuropsychopharmacology · doi:10.1093/ijnp/pyw014 · Cited by 59
Sundström, L., Myhre, S., Sundqvist, M., Ahnmark, A., McCoull, W., Raubo, P., Groombridge, S. D., Polla, M., Nyström, A.-C., Kristensson, L., et al. (2017) · PLOS ONE · doi:10.1371/journal.pone.0189060 · Cited by 53
Metadata
- Authors
- Shimpukade, B., Hudson, B. D., Hovgaard, C. K., Milligan, G., & Ulven, T.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-05-02
- Volume
- 55
- Issue
- 9
- Pages
- 4511-4515
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1969556083
- Cited by
- 162
- References
- 3
- FWCI
- 8.97
- Type
- journal article
- Language
- en
- Open access
- green
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- Shimpukade, B., Hudson, B. D., Hovgaard, C. K., Milligan, G., & Ulven, T. (2012). Discovery of a Potent and Selective GPR120 Agonist. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm300215x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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