Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2

P.C. Jensen, S Thiele, A Steen, A Elder, R Kolbeck, Sudip Ghosh, T M Frimurer, Mette Marie Rosenkilde

Research output: Contribution to journalJournal articleResearchpeer-review

17 Citations (Scopus)

Abstract

The majority of small molecule compounds targeting chemokine receptors share a similar pharmacophore with a centrally located aliphatic positive charge and flanking aromatic moieties. Here we describe a novel piperidine-based compound with structural similarity to previously described CCR8-specific agonists, but containing a unique phenyl-tetrazol moiety which, in addition to activity at CCR8 was also active at CCR1.
Original languageEnglish
JournalBritish Journal of Pharmacology
Volume166
Issue number1
Pages (from-to)258-75
Number of pages18
ISSN0007-1188
DOIs
Publication statusPublished - May 2012

Keywords

  • Animals
  • Binding Sites
  • COS Cells
  • Cercopithecus aethiops
  • Glutamic Acid
  • Humans
  • Inositol 1,4,5-Trisphosphate
  • Ligands
  • Models, Molecular
  • Piperidines
  • Point Mutation
  • Receptors, CCR1
  • Receptors, CCR8
  • Tetrazoles

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