A Brief Review of Drug Discovery Research for Human African Trypanosomiasis

被引：19

作者：

Cullen, Danica R. ^{[1
]}

Mocerino, Mauro ^{[1
]}

机构：

[1] Curtin Univ, Dept Chem, GPO Box U1987, Perth, WA, Australia

来源：

CURRENT MEDICINAL CHEMISTRY | 2017年 / 24卷 / 07期

关键词：

Human African Trypanosomiasis; Trypanosoma brucei; antitrypanosomal; drug discovery; phenotypic screening; target-based screening; N-MYRISTOYLTRANSFERASE INHIBITORS; TRYPANOCIDAL ACTIVITY; CLINICAL DEVELOPMENT; POTENT INHIBITORS; SLEEPING SICKNESS; LEAD COMPOUND; IN-VITRO; BRUCEI; DERIVATIVES; IDENTIFICATION;

D O I：

10.2174/0929867324666170120160034

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Human African Trypanosomiasis (HAT), a neglected disease endemic in SubSaharan 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.

引用

页码：701 / 717

页数：17