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寄生虫组蛋白修饰作为药物靶点。

Modifications of histones in parasites as drug targets.

机构信息

Key Laboratory of Animal Parasitology of Ministry of Agriculture, Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Shanghai 200241, China.

Key Laboratory of Animal Parasitology of Ministry of Agriculture, Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Shanghai 200241, China.

出版信息

Vet Parasitol. 2020 Feb;278:109029. doi: 10.1016/j.vetpar.2020.109029. Epub 2020 Jan 15.

Abstract

Post-translational modifications of histones and histone modifying enzymes play important roles in gene regulations and other physiological processes in parasites. Inhibitors of such modifying enzymes could be useful as novel therapeutics against parasitic diseases or as chemical probes for investigation of epigenetics. Development of parasitic histone modulators has got rapid expansion in the last few years. A number of highly potent and selective compounds have been reported, together with extensive preclinical studies of their biological activity. Some of these compounds have been widely used in humans targeting cancer and are found non-toxic. This review summarizes the antiparasitic activities of histone and histone modifying enzymes inhibitors evaluated in last few years. As the current chemotherapy against parasites is still not satisfactory, therefore, such compounds represents good starting points for the discovery of effective antiparasitic drugs.

摘要

组蛋白和组蛋白修饰酶的翻译后修饰在寄生虫的基因调控和其他生理过程中发挥着重要作用。这些修饰酶的抑制剂可用作抗寄生虫疾病的新型治疗药物,也可用作研究表观遗传学的化学探针。近年来,寄生虫组蛋白调节剂的开发取得了快速发展。已经报道了许多高活性和选择性的化合物,并对其生物学活性进行了广泛的临床前研究。其中一些化合物已被广泛用于人类的癌症治疗,且被发现无毒。本文综述了近年来评估的组蛋白和组蛋白修饰酶抑制剂的抗寄生虫活性。由于目前针对寄生虫的化疗仍不理想,因此,这些化合物是发现有效抗寄生虫药物的良好起点。

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