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The antimalarial screening landscape-looking beyond the asexual blood stage.
Current Opinion in Chemical Biology ( IF 7.8 ) Pub Date : 2019-03-16 , DOI: 10.1016/j.cbpa.2019.01.029
Sabrina Yahiya 1 , Ainoa Rueda-Zubiaurre 2 , Michael J Delves 3 , Matthew J Fuchter 2 , Jake Baum 1
Affiliation  

In recent years, the research agenda to tackle global morbidity and mortality from malaria disease has shifted towards innovation, in the hope that efforts at the frontiers of scientific research may re-invigorate gains made towards eradication. Discovery of new antimalarial drugs with novel chemotypes or modes of action lie at the heart of these efforts. There is a particular interest in drug candidates that target stages of the malaria parasite lifecycle beyond the symptomatic asexual blood stages. This is especially important given the spectre of emerging drug resistance to all current frontline antimalarials. One approach gaining increased interest is the potential of designing novel drugs that target parasite passage from infected individual to feeding mosquito and back again. Action of such therapeutics is geared much more at the population level rather than just concerned with the infected individual. The search for novel drugs active against these stages has been helped by improvements to in vitro culture of transmission and pre-erythrocytic parasite lifecycle stages, robotic automation and high content imaging, methodologies that permit the high-throughput screening (HTS) of compound libraries for drug discovery. Here, we review recent advances in the antimalarial screening landscape, focussed on transmission blocking as a key aim for drug-treatment campaigns of the future.

中文翻译:

进行抗疟疾筛查的目的是超越无性血液阶段。

近年来,解决全球疟疾发病率和死亡率的研究议程已转向创新,希望在科学研究前沿的努力可以重新激发消灭疟疾的成果。这些努力的核心是发现具有新化学类型或作用方式的抗疟药。候选药物对有症状的无性血液阶段以外的疟疾寄生虫生命周期的阶段特别感兴趣。考虑到对所有当前一线抗疟药产生耐药性的担忧,这一点尤其重要。一种引起人们越来越多兴趣的方法是设计新药的潜力,该药的目标是使寄生虫从受感染的人传播到喂养蚊子并再次传播。这种疗法的作用更多地是针对人群,而不仅仅是与受感染的个体有关。通过改进传播和前红细胞寄生虫生命周期各阶段的体外培养,机器人自动化和高内涵成像,允许对化合物库进行高通量筛选(HTS)的方法,有助于寻找对这些阶段有活性的新药。药物发现。在这里,我们回顾了抗疟药物筛查领域的最新进展,重点是阻断传播,将其作为未来药物治疗运动的主要目标。机器人自动化和高内涵成像,允许对化合物库进行高通量筛选(HTS)以便进行药物发现的方法。在这里,我们回顾了抗疟药物筛查领域的最新进展,重点是阻断传播,将其作为未来药物治疗运动的主要目标。机器人自动化和高内涵成像,允许对化合物库进行高通量筛选(HTS)以便进行药物发现的方法。在这里,我们回顾了抗疟药物筛查领域的最新进展,重点是阻断传播,将其作为未来药物治疗运动的主要目标。
更新日期:2019-11-01
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