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

Research output: Contribution to journalJournal articleResearchpeer-review

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

    Research areas

  • 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

ID: 48972161