Chemokine receptor antagonists: part 2.
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
This second part of the series concludes the review by describing antagonists for CCR5, CCR8, CCR9, CXCR3, CXCR4, and promiscuous antagonists.


CONCLUSIONS
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.
Faculty of Medicine National Heart and Lung Institute, Imperial College of Science, Technology & Medicine, Leukocyte Biology Section, London, UK. j.pease@imperial.ac.uk
James E
JE
Pease
Richard
R
Horuk
D000818:Animals; D065100:CCR5 Receptor Antagonists; D016503:Drug Delivery Systems; D006801:Humans; D010330:Patents as Topic; D054388:Receptors, CCR / Q000037:antagonists & inhibitors*; D054401:Receptors, CCR8 / Q000037:antagonists & inhibitors; D054367:Receptors, CXCR3 / Q000037:antagonists & inhibitors*; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors*
C119309:CC chemokine receptor 9; D065100:CCR5 Receptor Antagonists; D054388:Receptors, CCR; D054401:Receptors, CCR8; D054367:Receptors, CXCR3; D019718:Receptors, CXCR4