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Drug targeting of one or more aminoacyl-tRNA synthetase in the malaria parasite Plasmodium falciparum
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-02-08 , DOI: 10.1016/j.drudis.2018.01.050
Yogavel Manickam , Rini Chaturvedi , Palak Babbar , Nipun Malhotra , Vitul Jain , Amit Sharma

Malaria remains a major infectious disease and, despite incidence reduction, it threatens resurgence in drug-resistant forms. Antimalarial drugs remain the mainstay of therapeutic options and hence there is a constant need to identify and validate new druggable targets. Plasmodium falciparum aminoacyl-tRNA synthetases (Pf-aaRSs) drive protein translation and are potent targets for development of next-generation antimalarials. Here, we detail advances made in structural-biology-based investigations in Pf-aaRSs and discuss their distribution of druggable pockets. This review establishes a platform for systematic experimental dissection of malarial parasite aaRSs as a new focus for sustained drug development efforts against malaria.



中文翻译:

疟原虫恶性疟原虫中一种或多种氨酰基-tRNA合成酶的药物靶向

疟疾仍然是一种主要的传染病,尽管发病率有所降低,但它仍以耐药性形式重新流行。抗疟药仍然是治疗选择的主要手段,因此始终需要确定和验证新的可药物治疗靶标。恶性疟原虫氨酰基-tRNA合成酶(Pf - aRSs)驱动蛋白质翻译,并且是开发下一代抗疟疾药物的有效靶标。在这里,我们详细介绍了PfaRSs中基于结构生物学的研究取得的进展,并讨论了它们在可药用囊袋中的分布。这项审查建立了一个平台,系统性地对疟原虫aaRSs进行实验解剖,将其作为持续研发抗疟疾工作的新重点。

更新日期:2018-02-08
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