ELR+ CXC chemokines and their receptors (CXC chemokine receptor 1 and CXC chemokine receptor 2) as new therapeutic targets

Pharmacol Ther. 2006 Oct;112(1):139-49. doi: 10.1016/j.pharmthera.2006.04.002. Epub 2006 May 23.


ELR+ CXC chemokines, by direct interaction with their cell surface receptors CXC chemokine receptor 1 (CXCR1) and CXC chemokine receptor 2 (CXCR2), are believed to be crucially involved in the direct migration and activation of leukocytes. ELR+ CXC chemokines are supposed to play a key role in several inflammatory diseases and this makes ELR+ CXC chemokines and their receptors attractive therapeutic targets. The first aim of this review is to discuss the potential pathological role of ELR+ CXC chemokines in different pathologies, including ulcerative colitis (UC), ischaemia/reperfusion injury (RI), bronchiolitis obliterans syndrome (BOS) and tumor progression. Moreover, the most recently described inhibitors of ELR+ CXC chemokines and their therapeutic indications will be reviewed. Finally, the mode of action and the potential therapeutical use of reparixin, a new potent and selective inhibitor of CXCR1/2 activity, and its chemical derivatives are also discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Bronchiolitis Obliterans / drug therapy
  • Bronchiolitis Obliterans / metabolism
  • Chemokines, CXC / antagonists & inhibitors*
  • Chemokines, CXC / metabolism
  • Colitis, Ulcerative / drug therapy
  • Colitis, Ulcerative / metabolism
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Receptors, Interleukin-8A / antagonists & inhibitors*
  • Receptors, Interleukin-8A / metabolism
  • Receptors, Interleukin-8B / antagonists & inhibitors*
  • Receptors, Interleukin-8B / metabolism
  • Reperfusion Injury / drug therapy
  • Reperfusion Injury / metabolism


  • Chemokines, CXC
  • Receptors, Interleukin-8A
  • Receptors, Interleukin-8B