Discovery of Natural Phenols as G Protein-Coupled Receptor-35 (GPR35) Agonists

被引:26
|
作者
Deng, Huayun [1 ]
Hu, Haibei [1 ]
Ling, Shizhang [1 ]
Ferrie, Ann M. [1 ]
Fang, Ye [1 ]
机构
[1] Corning Inc, Biochem Technol Sci & Technol Div, Corning, NY 14831 USA
来源
ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 02期
关键词
GPR35; natural phenols; ellagic acid; biased agonism; ACID; PRODUCTS; DRUGS; IDENTIFICATION; CELLS;
D O I
10.1021/ml2003058
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report the discovery and characterization of natural phenols as G protein-coupled receptor-35 (GPR35) agonists. Pharmacological characterization using label-free dynamic mass redistribution and Tango beta-arrestin translocation assays revealed that GPR35-active natural phenols are divergent in their biased agonism.
引用
收藏
页码:165 / 169
页数:5
相关论文
共 50 条
  • [21] G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease
    Divorty, Nina
    Mackenzie, Amanda E.
    Nicklin, Stuart A.
    Milligan, Graeme
    FRONTIERS IN PHARMACOLOGY, 2015, 6
  • [22] Diindolylmethane Derivatives: Potent Agonists of the Immunostimulatory Orphan G Protein-Coupled Receptor GPR84
    Pillaiyar, Thanigaimalai
    Koese, Meryem
    Sylvester, Katharina
    Weighardt, Heike
    Thimm, Dominik
    Borges, Gleice
    Foerster, Irmgard
    von Kuegelgen, Ivar
    Mueller, Christa E.
    JOURNAL OF MEDICINAL CHEMISTRY, 2017, 60 (09) : 3636 - 3655
  • [23] Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD
    Song, Zhaoxiang
    Lu, Dan
    Sun, Jun
    Ye, Yangliang
    Fang, Jiahui
    Wang, Kai
    Guo, Shimeng
    Zhang, Qing
    He, Xinheng
    Xie, Xin
    Shen, Jianhua
    BIOORGANIC & MEDICINAL CHEMISTRY, 2023, 96
  • [24] Quantum Dot-Based Screening System for Discovery of G Protein-Coupled Receptor Agonists
    Lee, Junghan
    Kwon, Yong-Jun
    Choi, Youngseon
    Kim, Hi Chul
    Kim, Keumhyun
    Kim, JinYeop
    Park, Sun
    Song, Rita
    CHEMBIOCHEM, 2012, 13 (10) : 1503 - 1508
  • [25] Discovery and characterization of novel small-molecule agonists of G protein-coupled receptor 119
    Zhang, Shu-yong
    Li, Jing
    Xie, Xin
    ACTA PHARMACOLOGICA SINICA, 2014, 35 (04) : 540 - 548
  • [26] The Antiallergic Mast Cell Stabilizers Lodoxamide and Bufrolin as the First High and Equipotent Agonists of Human and Rat GPR35
    MacKenzie, Amanda E.
    Caltabiano, Gianluigi
    Kent, Toby C.
    Jenkins, Laura
    McCallum, Jennifer E.
    Hudson, Brian D.
    Nicklin, Stuart A.
    Fawcett, Lindsay
    Markwick, Rachel
    Charlton, Steven J.
    Milligan, Graeme
    MOLECULAR PHARMACOLOGY, 2014, 85 (01) : 91 - 104
  • [27] The G Protein-Coupled Receptor GPR17: Overview and Update
    Marucci, Gabriella
    Dal Ben, Diego
    Lambertucci, Catia
    Santinelli, Claudia
    Spinaci, Andrea
    Thomas, Ajiroghene
    Volpini, Rosaria
    Buccioni, Michela
    CHEMMEDCHEM, 2016, 11 (23) : 2567 - 2574
  • [28] Discovery and Cardioprotective Effects of the First Non-Peptide Agonists of the G Protein-Coupled Prokineticin Receptor-1
    Gasser, Adeline
    Brogi, Simone
    Urayama, Kyoji
    Nishi, Toshishide
    Kurose, Hitoshi
    Tafi, Andrea
    Ribeiro, Nigel
    Desaubry, Laurent
    Nebigil, Canan G.
    PLOS ONE, 2015, 10 (04):
  • [29] 6-Bromo-8-(4-[3H]methoxybenzamido)-4-oxo-4H-chromene-2-carboxylic Acid: A Powerful Tool for Studying Orphan G Protein-Coupled Receptor GPR35
    Thimm, Dominik
    Funke, Mario
    Meyer, Anne
    Mueller, Christa E.
    JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (17) : 7084 - 7099
  • [30] Pharmacology and function of the orphan GPR139 G protein-coupled receptor
    Vedel, Line
    Nohr, Anne Cathrine
    Gloriam, David E.
    Brauner-Osborne, Hans
    BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY, 2020, 126 : 35 - 46