CCR1 and CCR2 Antagonists

Author(s): Henning W. Zimmermann, Viktor Sterzer, Hacer Sahin

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 13 , 2014

Become EABM
Become Reviewer
Call for Editor

Graphical 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.

Keywords: CCR1, CCR2, chemokine receptors, clinical trials, disease, small molecule antagonists.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2014
Published on: 03 September, 2014
Page: [1539 - 1552]
Pages: 14
DOI: 10.2174/1568026614666140827144115
Price: $65

Article Metrics

PDF: 95