Centre for Medicinal Chemistry, School of Chemistry, University of Wollongong , Wollongong, 2522, Australia.
J Med Chem. 2014 Feb 27;57(4):1147-66. doi: 10.1021/jm400460d. Epub 2013 Oct 23.
Chikungunya virus is an emerging arbovirus that is widespread in tropical regions and is spreading quickly to temperate climates with recent epidemics in Africa and Asia and documented outbreaks in Europe and the Americas. It is having an increasingly major impact on humankind, with potentially life-threatening and debilitating arthritis. There is no treatment available, and only in the past 24 months have lead compounds for development as potential therapeutics been reported. This Perspective discusses the chikungunya virus as a significant, new emerging topic for medicinal chemistry, highlighting the key viral target proteins and their molecular functions that can be used in drug design, as well as the most important ongoing developments for anti-chikungunya virus research. It represents a complete picture of the current medicinal chemistry of chikungunya, supporting the development of chemotherapeutics through drug discovery and design targeting this virus.
基孔肯雅热病毒是一种新兴的虫媒病毒,广泛分布于热带地区,并且随着最近在非洲和亚洲的流行以及在欧洲和美洲有记录的暴发,正在迅速传播到温带气候地区。它对人类的影响越来越大,可能导致危及生命和使人虚弱的关节炎。目前尚无治疗方法,而且直到过去 24 个月才报告了开发潜在治疗方法的先导化合物。本文着眼于基孔肯雅热病毒,认为它是药物化学领域一个重要的新兴主题,重点介绍了可用于药物设计的关键病毒靶蛋白及其分子功能,以及抗基孔肯雅热病毒研究的最重要的最新进展。本文全面介绍了基孔肯雅热的药物化学,通过针对该病毒的药物发现和设计支持开发化学疗法。