Abstract

CC chemokines and their receptors play a key role in mediating both physiological and pathological processes. Chemokine receptors have been widely recognized as attractive drug targets by the pharmaceutical industry. A number of small molecule chemokine receptor antagonists have been developed for different disease indications, including rheumatoid arthritis (RA). This article describes the pharmacological evidence to support the therapeutic potential of targeting chemokine receptors, and highlights some of the recent progress in the field of developing small molecule antagonists for CC chemokine receptors aiming for RA and other disease applications. Furthermore, with the unsatisfactory clinical success so far, potential solutions leading to better success rates are also discussed.

Keywords: CC chemokines, CCR1, CCR2, CCR5, CCR6, Small molecule antagonist, Rheumatoid arthritis