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

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

Journal of medicinal chemistry (2008-11-15)
Takayoshi Suzuki, 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.

MATERIALS
Product Number
Brand
Product Description

Supelco
Linolenic acid, analytical standard
Sigma-Aldrich
Linolenic acid, ≥99%
Sigma-Aldrich
Linolenic acid, ~70% (GC)