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确定抗寄生虫化合物的靶点。

Defining the targets of antiparasitic compounds.

作者信息

Skinner-Adams Tina S, Sumanadasa Subathdrage D M, Fisher Gillian M, Davis Rohan A, Doolan Denise L, Andrews Katherine T

机构信息

Eskitis Institute for Drug Discovery, Griffith University, Nathan, Queensland 4121, Australia.

Eskitis Institute for Drug Discovery, Griffith University, Nathan, Queensland 4121, Australia.

出版信息

Drug Discov Today. 2016 May;21(5):725-39. doi: 10.1016/j.drudis.2016.01.002. Epub 2016 Jan 16.

DOI:10.1016/j.drudis.2016.01.002
PMID:26784142
Abstract

The treatment of major human parasitic infections is dependent on drugs that are plagued by issues of drug resistance. New chemotherapeutics with novel mechanisms of action (MOA) are desperately needed to combat multi-drug-resistant parasites. Although widespread screening strategies are identifying potential new hits for development against most major human parasitic diseases, in many cases such efforts are hindered by limited MOA data. Although MOA data are not essential for drug development, they can facilitate compound triage and provide a mechanism to combat drug resistance. Here we describe and discuss methods currently used to identify the targets of antiparasitic compounds, which could circumvent this bottleneck and facilitate the development of new antiparasitic drugs.

摘要

人类主要寄生虫感染的治疗依赖于存在耐药性问题的药物。迫切需要具有新型作用机制(MOA)的新型化学治疗药物来对抗多重耐药寄生虫。尽管广泛的筛选策略正在识别针对大多数主要人类寄生虫病进行开发的潜在新靶点,但在许多情况下,此类努力因作用机制数据有限而受阻。虽然作用机制数据对于药物开发并非必不可少,但它们可以促进化合物筛选,并提供一种对抗耐药性的机制。在这里,我们描述并讨论目前用于识别抗寄生虫化合物靶点的方法,这些方法可以绕过这一瓶颈并促进新型抗寄生虫药物的开发。

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