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Leishmaniasis drug discovery: recent progress and challenges in assay development
Drug Discovery Today ( IF 7.4 ) Pub Date : 2017-06-21 , DOI: 10.1016/j.drudis.2017.06.004
Bilal Zulfiqar , Todd B. Shelper , Vicky M. Avery

Leishmaniasis, caused by the trypanosomatid protozoan Leishmania, is endemic in 98 countries worldwide, with morbidity and mortality increasing daily. Despite available drugs, leishmaniasis faces the challenge of emerging resistance and toxicity concerns for current drug regimes. Identification of anti-leishmanial compounds representing new chemistry and novel mechanisms of action is essential to populate the drug discovery pipeline. The in vitro assays currently available have shown poor translational outcomes, with high compound attrition rates. It is therefore imperative that more physiologically relevant assays are developed to identify anti-leishmanial compounds. This review provides an overview of the disease, current treatment options and compares the various technologies and assay formats currently available for leishmanial drug discovery.



中文翻译:

利什曼病的药物发现:测定开发的最新进展和挑战

由锥虫原虫利什曼原虫引起的利什曼病在全世界98个国家流行,发病率和死亡率每天都在增加。尽管有可用的药物,利什曼病仍面临当前药物治疗中出现的新的耐药性和毒性问题的挑战。鉴定代表新化学方法和新作用机制的抗利什曼肽化合物对于填充药物开发管道至关重要。在体外当前可用的测定法显示翻译结果差,化合物损耗率高。因此,必须开发更多生理相关的测定法以鉴定抗利什曼肽化合物。这篇综述概述了该疾病,当前的治疗选择,并比较了目前可用于利什曼病药物发现的各种技术和测定形式。

更新日期:2017-06-21
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