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 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Journal of Medicinal Chemistry
Vol/bind	51
Udgave nummer	22
Sider (fra-til)	7061-4
Antal sider	4
ISSN	0022-2623
DOI	https://doi.org/10.1021/jm8010178
Status	Udgivet - 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.

I: Journal of Medicinal Chemistry, Bind 51, Nr. 22, 27.11.2008, s. 7061-4.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › 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, bind 51, nr. 22, s. 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.",

author = "Elisabeth Christiansen and Christian Urban and Nicole Merten and Kathrin Liebscher and Karlsen, {Kasper Kanneg{\aa}rd} and Alexandra Hamacher and Andreas Spinrath and Bond, {Andrew D} and Christel Drewke and Susanne Ullrich and Kassack, {Matthias U} and Evi Kostenis and Trond Ulven",

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AU - Christiansen, Elisabeth

AU - Urban, Christian

AU - Merten, Nicole

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

PY - 2008/11/27

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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.

U2 - 10.1021/jm8010178

DO - 10.1021/jm8010178

M3 - Journal article

C2 - 18947221

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JF - Journal of Medicinal Chemistry

IS - 22

ER -

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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