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潜在的治疗靶点以及技术在开发新型抗利什曼原虫药物中的作用。

Potential therapeutic targets and the role of technology in developing novel antileishmanial drugs.

作者信息

Rajasekaran Rajalakshmi, Chen Yi-Ping Phoebe

机构信息

College of Science, Health and Engineering, La Trobe University, Melbourne, VIC, Australia.

College of Science, Health and Engineering, La Trobe University, Melbourne, VIC, Australia.

出版信息

Drug Discov Today. 2015 Aug;20(8):958-68. doi: 10.1016/j.drudis.2015.04.006. Epub 2015 Apr 29.

Abstract

Leishmaniasis is the most prevalent pathogenic disease in many countries around the world, but there are few drugs available to treat it. Most antileishmanial drugs available are highly toxic, have resistance issues or require hospitalization for their use; therefore, they are not suitable for use in most of the affected countries. Over the past decade, the completion of the genomes of many human pathogens, including that of Leishmania spp., has opened new doors for target identification and validation. Here, we focus on the potential drug targets that can be used for the treatment of leishmaniasis and bring to light how recent technological advances, such as structure-based drug design, structural genomics, and molecular dynamics (MD), can be used to our advantage to develop potent and affordable antileishmanial drugs.

摘要

利什曼病是世界上许多国家最普遍的致病性疾病,但可用于治疗该病的药物很少。现有的大多数抗利什曼病药物毒性很高、存在耐药性问题或使用时需要住院治疗;因此,它们不适用于大多数受影响的国家。在过去十年中,包括利什曼原虫属在内的许多人类病原体基因组的完成,为靶点识别和验证打开了新的大门。在这里,我们重点关注可用于治疗利什曼病的潜在药物靶点,并揭示如何利用基于结构的药物设计、结构基因组学和分子动力学(MD)等最新技术进展来开发有效且价格合理的抗利什曼病药物。

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