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

@article{Suzuki2008IdentificationOG,
  title={Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists.},
  author={T. Suzuki and Sou-ichi Igari and A. Hirasawa and Mie Hata and M. Ishiguro and Hiroki Fujieda and Yukihiro Itoh and Tatsuya Hirano and H. Nakagawa and M. Ogura and M. Makishima and G. Tsujimoto and N. Miyata},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 23},
  pages={
          7640-4
        }
}
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. 
Discovery of a potent and selective GPR120 agonist.
TLDR
Optimization led to the discovery of the first potent and selective GPR120 agonist, which is hindered by the lack of suitable receptor modulators. Expand
Discovery and characterization of novel smallmolecule agonists of G protein-coupled receptor 119
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Three novel small-molecule GPR119 agonists with high receptor selectivity and capacity to induce GSIS in vitro were discovered and are potential candidates to be structurally optimized into drugs for the treatment of type 2 diabetes. Expand
Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation
TLDR
It is shown that a docking simulation using a GPR120 homology model might be useful to predict the agonistic activity of compounds. Expand
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TLDR
The mechanisms of signal transduction through GPR120 receptor, and discovery and development of GPR 120 agonists thereof are summarized. Expand
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Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.
TLDR
The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice, and deserves further biological evaluation and structural modifications. Expand
FFA 4 / GPR 120 : Pharmacology and Therapeutic Opportunities
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The Pharmacology of TUG-891, a Potent and Selective Agonist of the Free Fatty Acid Receptor 4 (FFA4/GPR120), Demonstrates Both Potential Opportunity and Possible Challenges to Therapeutic Agonism
TUG-891 [3-(4-((4-fluoro-4′-methyl-[1,1′-biphenyl]-2-yl)methoxy)phenyl)propanoic acid] was recently described as a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4Expand
Complex Pharmacology of Free Fatty Acid Receptors.
TLDR
The FFA family of receptors is a recently deorphanized set of GPCRs, the members of which are now receiving substantial interest as novel targets for the treatment of metabolic and inflammatory diseases. Expand
FFA1‐selective agonistic activity based on docking simulation using FFA1 and GPR120 homology models
TLDR
The FFA1 receptor and GPR120 are GPCRs whose endogenous ligands are medium‐ and long‐chain FFAs, and they are important in regulating insulin and GLP‐1 secretion respectively. Expand
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