Literature DB >> 29259758

SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.

Dong-Oh Yoon1, Xiaodi Zhao1, Dohyun Son1, Jung Tae Han1, Jaesook Yun1, Dongyun Shin2, Hyun-Ju Park1.   

Abstract

G-protein coupled receptor 40 (GPR40) has been considered to be an attractive drug target for the treatment of type 2 diabetes because of its role in free fatty acids-mediated enhancement of glucose-stimulated insulin secretion (GSIS) from pancreatic β-cells. A series of indole-5-propanoic acid compounds were synthesized, and their GPR40 agonistic activities were evaluated by nuclear factor of activated T-cells reporter assay and GSIS assay in the MIN-6 insulinoma cells. Three compounds, 8h (EC50 = 58.6 nM), 8i (EC50 = 37.8 nM), and 8o (EC50 = 9.4 nM), were identified as potent GPR40 agonists with good GSIS effects.

Entities:  

Year:  2017        PMID： 29259758      PMCID： PMC5733302          DOI： 10.1021/acsmedchemlett.7b00460

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  27 in total

1.  Fasiglifam (TAK-875) Inhibits Hepatobiliary Transporters: A Possible Factor Contributing to Fasiglifam-Induced Liver Injury.

Authors:  Xiuli Li; Kan Zhong; Zitao Guo; Dafang Zhong; Xiaoyan Chen
Journal:  Drug Metab Dispos       Date:  2015-08-14       Impact factor: 3.922

2.  Cl-pi interactions in protein-ligand complexes.

Authors:  Yumi N Imai; Yoshihisa Inoue; Isao Nakanishi; Kazuo Kitaura
Journal:  Protein Sci       Date:  2008-04-23       Impact factor: 6.725

3.  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

4.  The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).

Authors:  Chafiq Hamdouchi; Steven D Kahl; Anjana Patel Lewis; Guemalli R Cardona; Richard W Zink; Keyue Chen; Thomas E Eessalu; James V Ficorilli; Marialuisa C Marcelo; Keith A Otto; Kelly L Wilbur; Jayana P Lineswala; Jared L Piper; D Scott Coffey; Stephanie A Sweetana; Joseph V Haas; Dawn A Brooks; Edward J Pratt; Ruth M Belin; Mark A Deeg; Xiaosu Ma; Ellen A Cannady; Jason T Johnson; Nathan P Yumibe; Qi Chen; Pranab Maiti; Chahrzad Montrose-Rafizadeh; Yanyun Chen; Anne Reifel Miller
Journal:  J Med Chem       Date:  2016-11-11       Impact factor: 7.446

Review 5.  GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.

Authors:  Cheng Chen; He Li; Ya-Qiu Long
Journal:  Bioorg Med Chem Lett       Date:  2016-10-26       Impact factor: 2.823

6.  Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.

Authors:  Elisabeth Christiansen; Christian Urban; Manuel Grundmann; Maria E Due-Hansen; Ellen Hagesaether; Johannes Schmidt; Leonardo Pardo; Susanne Ullrich; Evi Kostenis; Matthias Kassack; Trond Ulven
Journal:  J Med Chem       Date:  2011-09-13       Impact factor: 7.446

7.  Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.

Authors:  Mikhail Krasavin; Alexey Lukin; Nikolay Zhurilo; Alexey Kovalenko; Ihor Zahanich; Sergey Zozulya; Daniel Moore; Irina G Tikhonova
Journal:  Bioorg Med Chem       Date:  2016-05-05       Impact factor: 3.641

8.  Fasiglifam (TAK-875) Alters Bile Acid Homeostasis in Rats and Dogs: A Potential Cause of Drug Induced Liver Injury.

Authors:  Francis S Wolenski; Andy Z X Zhu; Mike Johnson; Shaoxia Yu; Yuu Moriya; Takuya Ebihara; Vilmos Csizmadia; Jessica Grieves; Martin Paton; Mingxiang Liao; Christopher Gemski; Liping Pan; Majid Vakilynejad; Yvonne P Dragan; Swapan K Chowdhury; Patrick J Kirby
Journal:  Toxicol Sci       Date:  2017-05-01       Impact factor: 4.849

9.  A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.

Authors:  Chiori Yabuki; Hidetoshi Komatsu; Yoshiyuki Tsujihata; Risa Maeda; Ryo Ito; Kae Matsuda-Nagasumi; Kensuke Sakuma; Kazumasa Miyawaki; Naoya Kikuchi; Koji Takeuchi; Yugo Habata; Masaaki Mori
Journal:  PLoS One       Date:  2013-10-10       Impact factor: 3.240

10.  Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.

Authors:  Kae Nagasumi; Ritsuko Esaki; Kimihiko Iwachidow; Yoshitaka Yasuhara; Kazuhiro Ogi; Hideyuki Tanaka; Mitsugu Nakata; Takashi Yano; Kozo Shimakawa; Shigehisa Taketomi; Koji Takeuchi; Hiroyuki Odaka; Yoshihiko Kaisho
Journal:  Diabetes       Date:  2009-05       Impact factor: 9.461
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