Literature DB >> 18947221

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 Christiansen1, Christian Urban, Nicole Merten, Kathrin Liebscher, Kasper K Karlsen, Alexandra Hamacher, Andreas Spinrath, Andrew D Bond, Christel Drewke, Susanne Ullrich, Matthias U Kassack, Evi Kostenis, Trond Ulven.   

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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Year:  2008        PMID： 18947221     DOI： 10.1021/jm8010178

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  33 in total

1.  Deconvolution of complex G protein-coupled receptor signaling in live cells using dynamic mass redistribution measurements.

Authors:  Ralf Schröder; Nicole Janssen; Johannes Schmidt; Anna Kebig; Nicole Merten; Stephanie Hennen; Anke Müller; Stefanie Blättermann; Marion Mohr-Andrä; Sabine Zahn; Jörg Wenzel; Nicola J Smith; Jesús Gomeza; Christel Drewke; Graeme Milligan; Klaus Mohr; Evi Kostenis
Journal:  Nat Biotechnol       Date:  2010-08-15       Impact factor: 54.908

2.  Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells.

Authors:  Ralf Schröder; Johannes Schmidt; Stefanie Blättermann; Lucas Peters; Nicole Janssen; Manuel Grundmann; Wiebke Seemann; Dorina Kaufel; Nicole Merten; Christel Drewke; Jesus Gomeza; Graeme Milligan; Klaus Mohr; Evi Kostenis
Journal:  Nat Protoc       Date:  2011-10-20       Impact factor: 13.491

Review 3.  Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4.

Authors:  G Milligan; E Alvarez-Curto; K R Watterson; T Ulven; B D Hudson
Journal:  Br J Pharmacol       Date:  2015-02-27       Impact factor: 8.739

4.  Free fatty acid receptors: emerging targets for treatment of diabetes and its complications.

Authors:  Venkat Vangaveti; Venkatesh Shashidhar; Ghassan Jarrod; Bernhard T Baune; R Lee Kennedy
Journal:  Ther Adv Endocrinol Metab       Date:  2010-08       Impact factor: 3.565

5.  Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.

Authors:  Elisabeth Christiansen; Maria E Due-Hansen; Christian Urban; Nicole Merten; Michael Pfleiderer; Kasper K Karlsen; Sanne S Rasmussen; Mette Steensgaard; Alexandra Hamacher; Johannes Schmidt; Christel Drewke; Rasmus Koefoed Petersen; Karsten Kristiansen; Susanne Ullrich; Evi Kostenis; Matthias U Kassack; Trond Ulven
Journal:  ACS Med Chem Lett       Date:  2010-07-02       Impact factor: 4.345

6.  Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.

Authors:  Yingcai Wang; Jiwen Jim Liu; Paul J Dransfield; Liusheng Zhu; Zhongyu Wang; Xiaohui Du; Xianyun Jiao; Yongli Su; An-Rong Li; Sean P Brown; Annie Kasparian; Marc Vimolratana; Ming Yu; Vatee Pattaropong; Jonathan B Houze; Gayathri Swaminath; Thanhvien Tran; Khanh Nguyen; Qi Guo; Jane Zhang; Run Zhuang; Frank Li; Lynn Miao; Michael D Bartberger; Tiffany L Correll; David Chow; Simon Wong; Jian Luo; Daniel C-H Lin; Julio C Medina
Journal:  ACS Med Chem Lett       Date:  2013-05-07       Impact factor: 4.345

7.  A biased ligand for OXE-R uncouples Gα and Gβγ signaling within a heterotrimer.

Authors:  Stefanie Blättermann; Lucas Peters; Philipp Aaron Ottersbach; Andreas Bock; Viktoria Konya; C David Weaver; Angel Gonzalez; Ralf Schröder; Rahul Tyagi; Petra Luschnig; Jürgen Gäb; Stephanie Hennen; Trond Ulven; Leonardo Pardo; Klaus Mohr; Michael Gütschow; Akos Heinemann; Evi Kostenis
Journal:  Nat Chem Biol       Date:  2012-05-27       Impact factor: 15.040

Review 8.  Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3.

Authors:  Graeme Milligan; Leigh A Stoddart; Nicola J Smith
Journal:  Br J Pharmacol       Date:  2009-09       Impact factor: 8.739

9.  In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.

Authors:  C Urban; A Hamacher; H J Partke; M Roden; S Schinner; E Christiansen; M E Due-Hansen; T Ulven; H Gohlke; M U Kassack
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2013-07-17       Impact factor: 3.000

10.  The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1.

Authors:  Nicola J Smith; Leigh A Stoddart; Nicola M Devine; Laura Jenkins; Graeme Milligan
Journal:  J Biol Chem       Date:  2009-04-27       Impact factor: 5.157
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