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Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
Suzuki, Takayoshi; Igari, Sou-Ichi; Hirasawa, Akira; Hata, Mie; Ishiguro, Masaji; Fujieda, Hiroki; Itoh, Yukihiro; Hirano, Tatsuya; Nakagawa, Hidehiko; Ogura, Michitaka; Makishima, Makoto; Tsujimoto, Gozoh; Miyata, Naoki.
J Med Chem ; 51(23): 7640-4, 2008 Dec 11.
Article in English | MEDLINE | ID: mdl-19007110

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.


Subject(s)
Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , PPAR gamma/agonists , Receptors, G-Protein-Coupled/agonists , Binding Sites/drug effects , Carboxylic Acids/chemical synthesis , Crystallography, X-Ray , Dose-Response Relationship, Drug , Drug Design , Humans , Hydrogen Bonding , Models, Molecular , Molecular Structure , Stereoisomerism , Structure-Activity Relationship
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