Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2
Research output: Contribution to journal › Journal article › peer-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.
|Journal||British Journal of Pharmacology|
|Number of pages||18|
|Publication status||Published - May 2012|
- 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