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首页> 外文期刊>Drug design and discovery >Rational drug design using trypanothione reductase as a target for anti-trypanosomal and anti-leishmanial drug leads.
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Rational drug design using trypanothione reductase as a target for anti-trypanosomal and anti-leishmanial drug leads.

机译：使用锥虫硫磷还原酶作为抗锥虫和抗利什曼原虫药物靶标的合理药物设计。

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摘要

The parasite enzyme trypanothione reductase has been used as a target for rational drug design against trypanosomiasis and leishmaniasis in a number of laboratories. In this article the biochemical basis for its selection as a target is reviewed. The relevant structural aspects of the target are then compared with the homologous structure found in the mammalian hosts to indicate the molecular basis by which selective toxicity is likely to be achieved. An overview of known classes of inhibitors is provided, preparatory to a detailed coverage of approaches that have been taken to obtaining strong, selective inhibitors and the steps taken in the process of the initial discovery of tricyclic structures by interactive molecular graphics ligand design are outlined. Recent quantitative docking approaches which have been applied to this system are also described. Finally, the biological data of the activity against the various parasitic forms in vitro and in vivo are summarised.
机译：在许多实验室中，寄生虫酶锥虫硫磷还原酶已被用作针对锥虫病和利什曼病的合理药物设计的目标。在本文中，综述了选择其作为靶标的生化基础。然后将靶标的相关结构方面与哺乳动物宿主中发现的同源结构进行比较，以表明可能通过其实现选择性毒性的分子基础。提供了已知种类的抑制剂的概述，为获得强的选择性抑制剂所采取的方法的详细覆盖作了准备，并概述了通过交互式分子图形配体设计初步发现三环结构的过程中采取的步骤。还介绍了已应用于该系统的最新定量对接方法。最后，总结了体外和体内针对各种寄生虫形式的活性的生物学数据。

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