Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.
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.
Suzuki
Takayoshi
T
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
Igari
Sou-Ichi
S
Hirasawa
Akira
A
Hata
Mie
M
Ishiguro
Masaji
M
Fujieda
Hiroki
H
Itoh
Yukihiro
Y
Hirano
Tatsuya
T
Nakagawa
Hidehiko
H
Ogura
Michitaka
M
Makishima
Makoto
M
Tsujimoto
Gozoh
G
Miyata
Naoki
N
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
D002264:Carboxylic Acids; C519853:FFAR4 protein, human; D047495:PPAR gamma; D043562:Receptors, G-Protein-Coupled