Molecular requirements for inhibition of the chemokine receptor CCR8--probe-dependent allosteric interactions

Research output: Contribution to journalJournal articleResearchpeer-review

  • Pia Cwarzko Rummel
  • K N Arfelt
  • L Baumann
  • T J Jenkins
  • S Thiele
  • H R Lüttichau
  • A Johnsen
  • J Pease
  • S Ghosh
  • R Kolbeck
  • Rosenkilde, Mette
Here we present a novel series of CCR8 antagonists based on a naphthalene-sulfonamide structure. This structure differs from the predominant pharmacophore for most small-molecule CC-chemokine receptor antagonists, which in fact activate CCR8, suggesting that CCR8 inhibition requires alternative structural probes.
Original languageEnglish
JournalBritish Journal of Pharmacology
Volume167
Issue number6
Pages (from-to)1206-17
Number of pages12
ISSN0007-1188
DOIs
Publication statusPublished - Nov 2012

    Research areas

  • Animals, Binding Sites, Binding, Competitive, COS Cells, Cercopithecus aethiops, Chemokine CCL1, Chemokines, CC, Ligands, Naphthalenes, Receptors, CCR8, Viral Proteins

ID: 47965272