Title:CCR1 and CCR2 Antagonists
Volume: 14
Issue: 13
Author(s): Henning W. Zimmermann, Viktor Sterzer and Hacer Sahin
Affiliation:
Keywords:
CCR1, CCR2, chemokine receptors, clinical trials, disease, small molecule antagonists.
Abstract: Chemokines constitute a family of small heparin-binding proteins which orchestrate the infiltration of leukocytes
during inflammation, but also directly influence other physiological and pathophysiological processes. In humans,
more than 40 chemokines are known binding to around 18 G-protein-coupled receptors. A non-redundant role of certain
chemokines and their receptors has been identified within the last years in inflammation and host defense. Among
chemokine receptors, the CC chemokine receptors CCR1 and CCR2 have been shown to play a crucial role in these
processes. Importantly, these receptors have already been targeted by specific antagonists in early human trials for autoimmune
and infectious diseases. Although most of these antagonists failed to show any significant efficacy in the clinic,
the knowledge of their biological effects could henceforth offer new avenues with optimal strategies for producing successful
therapeutics.
