Literature DB >> 20064714

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Changyou Zhou1, Cheng Tang, Eric Chang, Min Ge, Songnian Lin, Eric Cline, Carina P Tan, Yue Feng, Yun-Ping Zhou, George J Eiermann, Aleksandr Petrov, Gino Salituro, Peter Meinke, Ralph Mosley, Taro E Akiyama, Monica Einstein, Sanjeev Kumar, Joel Berger, Andrew D Howard, Nancy Thornberry, Sander G Mills, Lihu Yang.   

Abstract

Systematic structure-activity relationship (SAR) studies of a screening lead led to the discovery of a series of thiazolidinediones (TZDs) as potent GPR40 agonists. Among them, compound C demonstrated an acute mechanism-based glucose-lowering in an intraperitoneal glucose tolerance test (IPGTT) in lean mice, while no effects were observed in GPR40 knock-out mice. Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 20064714     DOI: 10.1016/j.bmcl.2009.10.052

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


  16 in total

1.  Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist.

Authors:  Rieko Takano; Masao Yoshida; Masahiro Inoue; Takeshi Honda; Ryutaro Nakashima; Koji Matsumoto; Tatsuya Yano; Tsuneaki Ogata; Nobuaki Watanabe; Masakazu Hirouchi; Tomoko Yoneyama; Shuichiro Ito; Narihiro Toda
Journal:  ACS Med Chem Lett       Date:  2015-01-13       Impact factor: 4.345

Review 2.  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

3.  G Protein-coupled Receptor 40 (GPR40) and Peroxisome Proliferator-activated Receptor γ (PPARγ): AN INTEGRATED TWO-RECEPTOR SIGNALING PATHWAY.

Authors:  Shuibang Wang; Keytam S Awad; Jason M Elinoff; Edward J Dougherty; Gabriela A Ferreyra; Jennifer Y Wang; Rongman Cai; Junfeng Sun; Anetta Ptasinska; Robert L Danner
Journal:  J Biol Chem       Date:  2015-06-23       Impact factor: 5.157

4.  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

5.  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

6.  Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist.

Authors:  Sameer Agarwal; Santosh Sasane; Prashant Deshmukh; Bhadresh Rami; Debdutta Bandyopadhyay; Poonam Giri; Suresh Giri; Mukul Jain; Ranjit C Desai
Journal:  ACS Med Chem Lett       Date:  2016-09-21       Impact factor: 4.345

7.  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

Review 8.  PPARγ signaling and emerging opportunities for improved therapeutics.

Authors:  Shuibang Wang; Edward J Dougherty; Robert L Danner
Journal:  Pharmacol Res       Date:  2016-06-04       Impact factor: 7.658

Review 9.  Carboxylic acid (bio)isosteres in drug design.

Authors:  Carlo Ballatore; Donna M Huryn; Amos B Smith
Journal:  ChemMedChem       Date:  2013-01-29       Impact factor: 3.466

10.  An efficient multistep ligand-based virtual screening approach for GPR40 agonists.

Authors:  Sihui Yao; Tao Lu; Zifan Zhou; Haichun Liu; Haoliang Yuan; Ting Ran; Shuai Lu; Yanmin Zhang; Zhipeng Ke; Jinxing Xu; Xiao Xiong; Yadong Chen
Journal:  Mol Divers       Date:  2013-12-05       Impact factor: 2.943

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