Chemokine receptor antagonists: part 2

Abstract

Background: The first part of this two-part review discussed approaches to generating antagonists for some of the CC chemokine receptors, including CCR1, CCR2, CCR3, and CCR4. Objective/method: This second part of the series concludes the review by describing antagonists for CCR5, CCR8, CCR9, CXCR3, CXCR4, and promiscuous antagonists. Conclusion: Chemokine receptor antagonists have found mixed success as therapeutics. Although one antagonist – maraviroc, a CCR5 inhibitor to treat AIDS – has been registered as an approved drug, this is the only success so far. There have been many failures in the clinic and we discuss the idea of promiscuous receptor antagonists as an alternative approach.

Keywords::

• antagonism
• chemokine receptors
• chemokines
• GPCRs