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.
Duke Scholars
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Related Subject Headings
- beta-Arrestins
- Small Molecule Libraries
- Signal Transduction
- Receptors, G-Protein-Coupled
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Humans
- Drug Evaluation, Preclinical
- Drug Discovery
- Arrestins
Citation
Published In
DOI
EISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- beta-Arrestins
- Small Molecule Libraries
- Signal Transduction
- Receptors, G-Protein-Coupled
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Humans
- Drug Evaluation, Preclinical
- Drug Discovery
- Arrestins