Merck Research Laboratory, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. jinqi_liu@merck. com
Curr Top Med Chem. 2010;10(13):1250-67. doi: 10.2174/156802610791561192.
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.
CC 趋化因子及其受体在调节生理和病理过程中起着关键作用。趋化因子受体已被制药行业广泛认为是有吸引力的药物靶点。已经开发了许多小分子趋化因子受体拮抗剂用于不同的疾病适应症,包括类风湿关节炎(RA)。本文描述了支持靶向趋化因子受体治疗潜力的药理学证据,并强调了在开发用于 RA 和其他疾病应用的 CC 趋化因子受体小分子拮抗剂领域的一些最新进展。此外,鉴于迄今为止临床成功率不尽如人意,还讨论了一些可能提高成功率的解决方案。