Cullen Danica R, Mocerino Mauro
Department of Chemistry, Curtin University, GPO Box U1987, Perth WA. Australia.
Curr Med Chem. 2017;24(7):701-717. doi: 10.2174/0929867324666170120160034.
Human African Trypanosomiasis (HAT), a neglected disease endemic in Sub- Saharan Africa, is usually fatal if left untreated. It is caused by the parasite Trypanosoma brucei, and is spread by the tsetse fly. The drugs currently available to treat HAT are few, and limited in efficacy. Furthermore, resistance towards these drugs is beginning to grow. In the last 25 years, only one advance has been made into HAT treatment and consequently, there is an increasing need for new drugs to be sought that are able to effectively treat this disease. This review provides a brief overview of drug discovery research for HAT, focusing on research published in the last four years, identifying new molecules with the potential to be developed into anti-HAT agents. The methods of drug discovery have been grouped into three key areas; new molecules inspired by known antitrypanosomal agents, target-based screening, and phenotypic screening.
人类非洲锥虫病（HAT）是撒哈拉以南非洲地区流行的一种被忽视的疾病，如果不治疗通常会致命。它由布氏锥虫寄生虫引起，通过采采蝇传播。目前可用于治疗HAT的药物很少，且疗效有限。此外，对这些药物的耐药性开始增强。在过去25年里，HAT治疗仅取得了一项进展，因此，越来越需要寻找能够有效治疗这种疾病的新药。本综述简要概述了HAT的药物发现研究，重点关注过去四年发表的研究，识别有潜力开发成抗HAT药物的新分子。药物发现方法已分为三个关键领域：受已知抗锥虫药物启发的新分子、基于靶点的筛选和表型筛选。
