Tyrphostin analogs are GPR35 agonists

FEBS Lett. 2011 Jun 23;585(12):1957-62. doi: 10.1016/j.febslet.2011.05.026. Epub 2011 May 17.

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.

MeSH terms

  • Arrestins / metabolism
  • Drug Discovery / methods*
  • Endocytosis
  • Phosphorylation
  • Protein Kinase Inhibitors
  • Receptors, G-Protein-Coupled / agonists*
  • Tyrphostins / chemistry
  • Tyrphostins / pharmacology*
  • beta-Arrestins

Substances

  • Arrestins
  • GPR35 protein, human
  • Protein Kinase Inhibitors
  • Receptors, G-Protein-Coupled
  • Tyrphostins
  • beta-Arrestins