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Issue 10, 2012
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Discovery of nitrophenols as GPR35 agonists

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Abstract

GPR35 is a family A orphan G protein-coupled receptor whose biological functions are largely unknown. Identification of novel GPR35 ligands is essential to elucidate the biology and pathophysiology of GPR35. Here we report the discovery of nitrophenol compounds to be a novel chemical class of GPR35 agonists. Both endogenously and stably expressed GPR35 were found to be activated by a number of nitrophenol analogues including 2-amino-4,6-dinitrophenol, tolcapone and nitecapone. Among them, 4,4′-(2,2-dichloroethene-1,1-diyl)bis(2,6-dinitrophenol) was found to be the most potent GPR35 agonist.

Graphical abstract: Discovery of nitrophenols as GPR35 agonists

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Publication details

The article was received on 24 Jul 2012, accepted on 01 Aug 2012 and first published on 03 Aug 2012


Article type: Concise Article
DOI: 10.1039/C2MD20210G
Citation: Med. Chem. Commun., 2012,3, 1270-1274
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    Discovery of nitrophenols as GPR35 agonists

    H. Deng and Y. Fang, Med. Chem. Commun., 2012, 3, 1270
    DOI: 10.1039/C2MD20210G

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