title: Discovery of novel FFA4 (GPR120) receptor agonists with β-arrestin2-biased characteristics.
abstract: 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.
  
  
  CONCLUSIONS
  These compounds may serve as the useful toolkits for detecting differential biased mechanism and developing new candidate therapeutic agents of the FFA4 receptor.
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Ang
authors.initials: A
authors.lastname: Li
authors.affiliation: Department of Biochemistry & Molecular Biology, School of Medicine, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Duxiao
authors.initials: D
authors.lastname: Yang
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Mengyuan
authors.initials: M
authors.lastname: Zhu
authors.affiliation: National Research Institute of Chinese Medicine, Taipei 112, Taiwan.
authors.forename: Keng-chang
authors.initials: KC
authors.lastname: Tsai
authors.affiliation: Duke University, School of Medicine, Durham, NC 27705, USA.
authors.forename: Kun-hong
authors.initials: KH
authors.lastname: Xiao
authors.affiliation: Department of Biochemistry & Molecular Biology, School of Medicine, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Yu
authors.affiliation: Department of Biochemistry & Molecular Biology, School of Medicine, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Jinpeng
authors.initials: J
authors.lastname: Sun
authors.affiliation: Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University, Jinan, Shandong 250012, China.
authors.forename: Lupei
authors.initials: L
authors.lastname: Du
mesh_terms: D019390:Arrestins / Q000378:metabolism*; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology*; D000071557:beta-Arrestins
chemical_list: D019390:Arrestins; C519853:FFAR4 protein, human; D043562:Receptors, G-Protein-Coupled; D054852:Small Molecule Libraries; D000071557:beta-Arrestins