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- Title
Tyrphostin analogs are GPR35 agonists
- Authors
Deng, Huayun; Hu, Haibei; Fang, Ye
- Abstract
Abstract: 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.
- Subjects
PROTEIN-tyrosine kinases; G proteins; PHOSPHORYLATION; BIOSENSORS; CATECHOL; BIOLOGICAL assay; PHARMACOLOGY; CHROMOSOMAL translocation
- Publication
FEBS Letters, 2011, Vol 585, Issue 12, p1957
- ISSN
0014-5793
- Publication type
Article
- DOI
10.1016/j.febslet.2011.05.026