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New leads for drug repurposing against malaria
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-08-09 , DOI: 10.1016/j.drudis.2018.08.006
Nila Madassary Pazhayam , Jyoti Chhibber-Goel , Amit Sharma

Malaria is threatening a resurgence because of drug resistance against frontline artemisinin-based combination therapies (ACTs). This necessitates the development of alternate routes for malaria treatment. Here, we present a refined focus on US Food and Drug Administration (FDA)-approved over-the-counter (OTC) drugs that could be repurposed. We analyzed growth inhibition data for Plasmodium falciparum and Plasmodium berghei in the context of 189 and 37 drugs (total of 226), respectively. Of these, our analyses revealed 18 currently used drugs that would be suitable for further development as potential antimalarials. Eight identified drugs share enzymatic targets between the human host and the malaria parasite, providing a platform for mechanistic and drug selectivity studies that could provide optimized leads as next-generation antimalarials.



中文翻译:

疟疾药物重新利用的新线索

由于对基于青蒿素的前线联合疗法(ACTs)的耐药性,疟疾正在威胁死灰复燃。这就需要开发替代治疗疟疾的途径。在这里,我们重点介绍了美国食品药品监督管理局(FDA)批准的可以重新调整用途的非处方药(OTC)。我们分析了恶性疟原虫伯氏疟原虫的生长抑制数据分别涉及189种和37种药物(总共226种)。其中,我们的分析显示了18种目前正在使用的药物,这些药物适合作为潜在的抗疟药进行进一步开发。八种鉴定出的药物在人类宿主和疟疾寄生虫之间共享酶促靶标,为机理和药物选择性研究提供了平台,可以为下一代抗疟药提供优化的线索。

更新日期:2018-08-09
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