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Tyrphostin analogs are GPR35 agonists
Author(s) -
Deng Huayun,
Hu Haibei,
Fang Ye
Publication year - 2011
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2011.05.026
Subject(s) - internalization , receptor , microbiology and biotechnology , chemistry , phosphorylation , agonist , orphan receptor , kinase , biology , pharmacology , biochemistry , gene , transcription factor
GPR35 is an orphan G protein‐coupled receptor that is not well‐characterized. Here we employ dynamic mass redistribution (DMR) assays to discover new GPR35 agonists. DMR assays identified tyrphostin analogs as GPR35 agonists, which were confirmed with receptor internalization, Tango β‐arrestin translocation, and extracellular‐signal‐regulated kinase phosphorylation assays. These agonists provide pharmacological tools to study the biology and function of GPR35.