Literature DB >> 19007110

Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.

Takayoshi Suzuki1, Sou-Ichi Igari, Akira Hirasawa, Mie Hata, Masaji Ishiguro, Hiroki Fujieda, Yukihiro Itoh, Tatsuya Hirano, Hidehiko Nakagawa, Michitaka Ogura, Makoto Makishima, Gozoh Tsujimoto, Naoki Miyata.   

Abstract

A weak, nonselective G protein-coupled receptor 120 (GPR120) agonist 10 was found by screening a series of carboxylic acids derived from the peroxisome proliferator-activated receptor gamma (PPARgamma) agonist 3. Modification based on the homology model of GPR120 led to the first GPR120-selective agonist 12. These results provide a basis for constructing new tools for probing the biology of GPR120 and for developing new candidate therapeutic agents.

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Year:  2008        PMID： 19007110     DOI： 10.1021/jm800970b

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


  28 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.  Discovery and characterization of novel small molecule agonists of G protein-coupled receptor 119.

Authors:  Shu-yong Zhang; Jing Li; Xin Xie
Journal:  Acta Pharmacol Sin       Date:  2014-03-31       Impact factor: 6.150

3.  Differential signaling by splice variants of the human free fatty acid receptor GPR120.

Authors:  Sarah-Jane Watson; Alastair J H Brown; Nicholas D Holliday
Journal:  Mol Pharmacol       Date:  2012-01-26       Impact factor: 4.436

4.  Discovery of the First Environment-Sensitive Fluorescent Probe for GPR120 (FFA4) Imaging.

Authors:  Jiaxiang Liu; Chengsen Tian; Tianyu Jiang; Yuqi Gao; Yubin Zhou; Minyong Li; Lupei Du
Journal:  ACS Med Chem Lett       Date:  2017-03-27       Impact factor: 4.345

Review 5.  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

6.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

7.  Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.

Authors:  Xuqing Zhang; Chaozhong Cai; Zhihua Sui; Mark Macielag; Yuanping Wang; Wen Yan; Arthur Suckow; Hong Hua; Austin Bell; Peter Haug; Wilma Clapper; Celia Jenkinson; Joseph Gunnet; James Leonard; William V Murray
Journal:  ACS Med Chem Lett       Date:  2017-07-27       Impact factor: 4.345

8.  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

Review 9.  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

Review 10.  GPR120: a critical role in adipogenesis, inflammation, and energy metabolism in adipose tissue.

Authors:  Tongxing Song; Yang Yang; Yuanfei Zhou; Hongkui Wei; Jian Peng
Journal:  Cell Mol Life Sci       Date:  2017-03-11       Impact factor: 9.261
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