| Autor: |
Murakoshi, Michiko, Kuwabara, Harumi, Nagasaki, Miyuki, Xiong, Yu Mei, Reagan, Jeff D., Maeda, Hiroaki, Nara, Futoshi |
| Zdroj: |
Journal of Receptors & Signal Transduction; Jun2017, Vol. 37 Issue 3, p290-296, 7p |
| Abstrakt: |
GPR142 is a G-protein-coupled receptor (GPCR), whose most potent and efficacious ligand has been reported as being the natural amino acidl-tryptophan. GPR142 is highly expressed in pancreatic β-cells and immune cells, suggesting the receptor may play a role in the pathogenesis and development of diabetes or inflammatory diseases. In a previous report, we developed GPR142 agonists as insulin secretagogues. In this report, we show the discovery of a selective, potent small-molecule GPR142 antagonist, CLP-3094, and its pharmacological characteristics. These data support targeting this receptor for the treatment of chronic inflammatory diseases. [ABSTRACT FROM PUBLISHER] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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