title: Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Sou-Ichi
authors.initials: S
authors.lastname: Igari
authors.forename: Akira
authors.initials: A
authors.lastname: Hirasawa
authors.forename: Mie
authors.initials: M
authors.lastname: Hata
authors.forename: Masaji
authors.initials: M
authors.lastname: Ishiguro
authors.forename: Hiroki
authors.initials: H
authors.lastname: Fujieda
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Hirano
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Nakagawa
authors.forename: Michitaka
authors.initials: M
authors.lastname: Ogura
authors.forename: Makoto
authors.initials: M
authors.lastname: Makishima
authors.forename: Gozoh
authors.initials: G
authors.lastname: Tsujimoto
authors.forename: Naoki
authors.initials: N
authors.lastname: Miyata
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D006860:Hydrogen Bonding; D008958:Models, Molecular; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D002264:Carboxylic Acids; C519853:FFAR4 protein, human; D047495:PPAR gamma; D043562:Receptors, G-Protein-Coupled