Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

Elisabeth Christiansen; Christian Urban; Nicole Merten; Kathrin Liebscher; Kasper Kannegård Karlsen; Alexandra Hamacher; Andreas Spinrath; Andrew D Bond; Christel Drewke; Susanne Ullrich; Matthias U Kassack; Evi Kostenis; Trond Ulven

doi:10.1021/jm8010178

Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

Elisabeth Christiansen, Christian Urban, Nicole Merten, Kathrin Liebscher, Kasper Kannegård Karlsen, Alexandra Hamacher, Andreas Spinrath, Andrew D Bond, Christel Drewke, Susanne Ullrich, Matthias U Kassack, Evi Kostenis, Trond Ulven

106 Citations (Scopus)

Abstract

A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.

Original language	English
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	22
Pages (from-to)	7061-4
Number of pages	4
ISSN	0022-2623
DOIs	https://doi.org/10.1021/jm8010178
Publication status	Published - 27 Nov 2008

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10.1021/jm8010178

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Christiansen, E., Urban, C., Merten, N., Liebscher, K., Karlsen, K. K., Hamacher, A., Spinrath, A., Bond, A. D., Drewke, C., Ullrich, S., Kassack, M. U., Kostenis, E., & Ulven, T. (2008). Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. Journal of Medicinal Chemistry, 51(22), 7061-4. https://doi.org/10.1021/jm8010178

Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. / Christiansen, Elisabeth; Urban, Christian; Merten, Nicole et al.

In: Journal of Medicinal Chemistry, Vol. 51, No. 22, 27.11.2008, p. 7061-4.

Research output: Contribution to journal › Journal article › Research › peer-review

Christiansen, E, Urban, C, Merten, N, Liebscher, K, Karlsen, KK, Hamacher, A, Spinrath, A, Bond, AD, Drewke, C, Ullrich, S, Kassack, MU, Kostenis, E & Ulven, T 2008, 'Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes', Journal of Medicinal Chemistry, vol. 51, no. 22, pp. 7061-4. https://doi.org/10.1021/jm8010178

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abstract = "A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.",

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AU - Liebscher, Kathrin

AU - Karlsen, Kasper Kannegård

AU - Hamacher, Alexandra

AU - Spinrath, Andreas

AU - Bond, Andrew D

AU - Drewke, Christel

AU - Ullrich, Susanne

AU - Kassack, Matthias U

AU - Kostenis, Evi

AU - Ulven, Trond

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AB - A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.

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Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

Abstract

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