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首页> 外文期刊>Drug Target Insights >Trypanothione Reductase: A Viable Chemotherapeutic Target for Antitrypanosomal and Antileishmanial Drug Design
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Trypanothione Reductase: A Viable Chemotherapeutic Target for Antitrypanosomal and Antileishmanial Drug Design

机译：锥虫酮还原酶：一种抗锥虫和抗leishmanmanial药物设计的可行化学治疗目标。

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摘要

Trypanosomiasis and leishmaniasis are two debilitating disease groups caused by parasites of Trypanosoma and Leishmania spp. and affecting millions of people worldwide. A brief outline of the potential targets for rational drug design against these diseases are presented, with an emphasis placed on the enzyme trypanothione reductase. Trypanothione reductase was identified as unique to parasites and proposed to be an effective target against trypanosomiasis and leishmaniasis. The biochemical basis of selecting this enzyme as a target, with reference to the simile and contrast to human analogous enzyme glutathione reductase, and the structural aspects of its active site are presented. The process of designing selective inhibitors for the enzyme trypanothione reductase has been discussed. An overview of the different chemical classes of inhibitors of trypanothione reductase with their inhibitory activities against the parasites and their prospects as future chemotherapeutic agents are briefl y revealed.
机译：锥虫病和利什曼病是由锥虫和利什曼原虫属的寄生虫引起的两个使人衰弱的疾病组。并影响着全球数百万人。介绍了针对这些疾病的合理药物设计的潜在目标的简要概述，重点放在锥虫硫磷还原酶上。锥虫还原酶被认为是寄生虫所独有的，被认为是对抗锥虫病和利什曼病的有效靶点。介绍了选择该酶作为靶标的生化基础，并参考了人类类似酶谷胱甘肽还原酶的比喻和对比，以及其活性位点的结构方面。已经讨论了设计锥虫硫醚还原酶选择性抑制剂的过程。简要揭示了锥虫还原酶抑制剂的不同化学类别及其对寄生虫的抑制活性及其作为未来化学治疗剂的前景。

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