Literature DB >> 18993064

Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.

Sandip B Bharate1, Atish Rodge, Rajendra K Joshi, Jaspreet Kaur, Shaila Srinivasan, S Senthil Kumar, Asha Kulkarni-Almeida, Sarala Balachandran, Arun Balakrishnan, Ram A Vishwakarma.   

Abstract

In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxyls were synthesized and evaluated for GPR40 agonism using functional calcium-flux assay. Out of 17 compounds evaluated, 14, 17, 19 and 25 exhibited good GPR40 agonistic activity with EC(50) values ranging from 0.07 to 8 microM (pEC(50) 7.12-5.09), respectively, with maximal agonistic response of 84-102%.

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Year:  2008        PMID： 18993064     DOI： 10.1016/j.bmcl.2008.10.085

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

1.  FFA1-selective agonistic activity based on docking simulation using FFA1 and GPR120 homology models.

Authors:  Masato Takeuchi; Akira Hirasawa; Takafumi Hara; Ikuo Kimura; Tatsuya Hirano; Takayoshi Suzuki; Naoki Miyata; Takeo Awaji; Masaji Ishiguro; Gozoh Tsujimoto
Journal:  Br J Pharmacol       Date:  2013-04       Impact factor: 8.739

2.  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

3.  Analysis of hyperforin (St. John's wort) action at TRPC6 channel leads to the development of a new class of antidepressant drugs.

Authors:  Yamina El Hamdaoui; Fang Zheng; Nikolas Fritz; Lian Ye; Mai Anh Tran; Kevin Schwickert; Tanja Schirmeister; Albert Braeuning; Dajana Lichtenstein; Ute A Hellmich; Dorothee Weikert; Markus Heinrich; Giulia Treccani; Michael K E Schäfer; Gabriel Nowak; Bernd Nürnberg; Christian Alzheimer; Christian P Müller; Kristina Friedland
Journal:  Mol Psychiatry       Date:  2022-10-12       Impact factor: 13.437

Review 4.  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

5.  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

6.  Novel selective ligands for free fatty acid receptors GPR120 and GPR40.

Authors:  Takafumi Hara; Akira Hirasawa; Qi Sun; Keiko Sadakane; Chisato Itsubo; Tomoyo Iga; Tetsuya Adachi; Taka-aki Koshimizu; Toshihiro Hashimoto; Yoshinori Asakawa; Gozoh Tsujimoto
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2009-05-27       Impact factor: 3.000

Review 7.  Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes.

Authors:  Bo Ahrén
Journal:  Nat Rev Drug Discov       Date:  2009-04-14       Impact factor: 84.694

8.  AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents.

Authors:  Daniel C-H Lin; Jane Zhang; Run Zhuang; Frank Li; Kathy Nguyen; Michael Chen; Thanhvien Tran; Edwin Lopez; Jenny Ying Lin Lu; Xiaoyan Nina Li; Liang Tang; George R Tonn; Gayathri Swaminath; Jeff D Reagan; Jin-Long Chen; Hui Tian; Yi-Jyun Lin; Jonathan B Houze; Jian Luo
Journal:  PLoS One       Date:  2011-11-08       Impact factor: 3.752

Review 9.  Activation of GPR40 as a therapeutic target for the treatment of type 2 diabetes.

Authors:  Charles F Burant
Journal:  Diabetes Care       Date:  2013-08       Impact factor: 19.112

10.  Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.

Authors:  Daniel C-H Lin; Qi Guo; Jian Luo; Jane Zhang; Kathy Nguyen; Michael Chen; Thanh Tran; Paul J Dransfield; Sean P Brown; Jonathan Houze; Marc Vimolratana; Xian Yun Jiao; Yingcai Wang; Nigel J M Birdsall; Gayathri Swaminath
Journal:  Mol Pharmacol       Date:  2012-08-02       Impact factor: 4.054
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