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寄生性沉默调节蛋白2作为药物研发的一个契机。

Parasitic sirtuin 2 as an opportunity in drug discovery.

作者信息

Gomes Renan Augusto, Fornari Evelin, Silva Rocha Ana Carolina, Tripodi Gustavo Luis, Silva Emery Flavio da, Goulart Trossini Gustavo Henrique

机构信息

Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, Av. Prof. Lineu Prestes, 580, São Paulo, SP, 05508-000, Brasil.

Departamento de Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Av. do Café, s/n, Ribeirão Preto, SP, 14040-903, Brasil.

出版信息

Future Med Chem. 2021 Aug;13(16):1397-1409. doi: 10.4155/fmc-2021-0091. Epub 2021 Jun 30.

Abstract

Infections caused by protozoans remain a public health issue, especially in tropical countries. Serious adverse events, lack of efficacy at the different stages of the infection and routes of administration that have a negative impact on treatment adherence are some of the problems with currently available therapy against these diseases. Here we describe an epigenetic target, sirtuin 2 and its related proteins, that is promising given the results in phenotypic assays and models against Sir2 of , , , , and parasites. The results we present highlight how this target can be extensively explored and how its inhibitors might be employed in the clinic.

摘要

原生动物引起的感染仍然是一个公共卫生问题,尤其是在热带国家。严重不良事件、在感染不同阶段缺乏疗效以及给药途径对治疗依从性产生负面影响,是目前针对这些疾病的现有疗法存在的一些问题。在此,我们描述了一个表观遗传靶点——沉默调节蛋白2及其相关蛋白,鉴于在针对利什曼原虫、锥虫、疟原虫、贾第虫和隐孢子虫的Sir2的表型试验和模型中所取得的结果,该靶点颇具前景。我们展示的结果突出了该靶点如何能够得到广泛探索,以及其抑制剂如何可能应用于临床。

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