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Multi-target drugs active against leishmaniasis: A paradigm of drug repurposing.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2019-08-29 , DOI: 10.1016/j.ejmech.2019.111660 Susana Santos Braga 1
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2019-08-29 , DOI: 10.1016/j.ejmech.2019.111660 Susana Santos Braga 1
Affiliation
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This mini-review focuses on leishmanicidal drugs that were sourced from small molecules previously approved for other diseases. The mechanisms of action of these molecules are herein explored, to probe the origins of their inter-species growth inhibitory activities. It is shown how the transversal action of the azoles - fluconazole, posaconazole and itraconazole - in both fungi and Leishmania is due to the occurrence of the same target, lanosterol 14-α-demethylase, in these two groups of species. In turn, the drugs miltefosine and amphotericin B are presented as truly multi-target agents, acting on small molecules, proteins, genes and even organelles. Steps towards future leishmanicidal drug candidates based on the multi-target strategy and on drug repurposing are also briefly presented.
中文翻译：
对抗利什曼病的多靶点药物：改变药物用途的范例。
这篇小型综述重点关注从以前被批准用于其他疾病的小分子中提取的杀菌剂。本文探索了这些分子的作用机理，以探究其种间生长抑制活性的起源。结果表明，在这两组物种中，真菌和利什曼原虫中的吡唑类化合物（氟康唑，泊沙康唑和伊曲康唑）的横向作用是由于相同靶标羊毛甾醇14-α-脱甲基酶的发生而引起的。反过来，药物miltefosine和两性霉素B则是真正的多靶标药物，作用于小分子，蛋白质，基因甚至细胞器。还简要介绍了基于多目标策略和基于药物再利用的未来杀菌剂候选药物的步骤。
更新日期：2019-08-29
中文翻译：
对抗利什曼病的多靶点药物：改变药物用途的范例。
这篇小型综述重点关注从以前被批准用于其他疾病的小分子中提取的杀菌剂。本文探索了这些分子的作用机理，以探究其种间生长抑制活性的起源。结果表明，在这两组物种中，真菌和利什曼原虫中的吡唑类化合物（氟康唑，泊沙康唑和伊曲康唑）的横向作用是由于相同靶标羊毛甾醇14-α-脱甲基酶的发生而引起的。反过来，药物miltefosine和两性霉素B则是真正的多靶标药物，作用于小分子，蛋白质，基因甚至细胞器。还简要介绍了基于多目标策略和基于药物再利用的未来杀菌剂候选药物的步骤。
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