Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation

Research output: Contribution to journalJournal articleResearchpeer-review

  • Tau Benned-Jensen
  • Christian M Madsen
  • Kristine N Arfelt
  • Christian Smethurts
  • Andy Blanchard
  • Robert Jepras
  • Rosenkilde, Mette
The Epstein-Barr virus induced gene 2 (EBI2) was recently identified as the first oxysterol-activated 7TM receptor. EBI2 is essential for B cell trafficking within lymphoid tissues and thus the humoral immune response in general. Here we characterize the antagonism of the non-peptide molecule GSK682753A, which blocks oxysterol-induced G-protein activation, β-arrestin recruitment and B-cell chemotaxis. We furthermore demonstrate that activation triggers pertussis toxin-sensitive MAP kinase phosphorylation, which is also inhibited by GSK682753A. Thus, EBI2 signalling in B cells mediates key phenotypic functions via signalling pathways amenable to manipulation providing additional therapeutic options for inhibiting EBI2 activity.
Original languageEnglish
JournalFEBS Open Bio
Pages (from-to)156-60
Number of pages5
Publication statusPublished - 2013

ID: 48310696