Discovery of novel FFA4 (GPR120) receptor agonists with β-arrestin2-biased characteristics.
BACKGROUND: Free fatty acid 4 (FFA4) (GPR120) receptor functions as a receptor for unsaturated long-chain free fatty acids by regulating the secretion of glucagon-like peptide-1 and suppressing the inflammatory process, in which these two distinct biological functions are modulated by two signaling pathways, Gq and β-arrestin2, respectively. RESULTS: By using pharmacophore modeling and virtual screening methods, several compounds are found with excellent activities for agonizing FFA4 receptor. It needs to be noted that among them, some molecules demonstrate appealing β-arrestin2-biased properties for the FFA4 receptor. CONCLUSION: These compounds may serve as the useful toolkits for detecting differential biased mechanism and developing new candidate therapeutic agents of the FFA4 receptor.
Li, A; Yang, D; Zhu, M; Tsai, K-C; Xiao, K-H; Yu, X; Sun, J; Du, L
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