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

  • J Med Chem. 2008 Dec 11;51(23):7640-4. doi: 10.1021/jm800970b.
Takayoshi Suzuki  1 ,  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
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
PMID: 19007110 DOI: 10.1021/jm800970b
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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