Gaona-López Carlos, Vazquez-Jimenez Lenci K, Gonzalez-Gonzalez Alonzo, Delgado-Maldonado Timoteo, Ortiz-Pérez Eyrá, Nogueda-Torres Benjamín, Moreno-Rodríguez Adriana, Vázquez Karina, Saavedra Emma, Rivera Gildardo
Laboratorio de Biotecnología Farmacéutica, Centro de Biotecnología Genómica, Instituto Politécnico Nacional, Reynosa 88710, Mexico.
Departamento de Parasitología, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Mexico City 11340, Mexico.
Pharmaceuticals (Basel). 2023 Apr 4;16(4):543. doi: 10.3390/ph16040543.
Protozoan parasite diseases cause significant mortality and morbidity worldwide. Factors such as climate change, extreme poverty, migration, and a lack of life opportunities lead to the propagation of diseases classified as tropical or non-endemic. Although there are several drugs to combat parasitic diseases, strains resistant to routinely used drugs have been reported. In addition, many first-line drugs have adverse effects ranging from mild to severe, including potential carcinogenic effects. Therefore, new lead compounds are needed to combat these parasites. Although little has been studied regarding the epigenetic mechanisms in lower eukaryotes, it is believed that epigenetics plays an essential role in vital aspects of the organism, from controlling the life cycle to the expression of genes involved in pathogenicity. Therefore, using epigenetic targets to combat these parasites is foreseen as an area with great potential for development. This review summarizes the main known epigenetic mechanisms and their potential as therapeutics for a group of medically important protozoal parasites. Different epigenetic mechanisms are discussed, highlighting those that can be used for drug repositioning, such as histone post-translational modifications (HPTMs). Exclusive parasite targets are also emphasized, including the base J and DNA 6 mA. These two categories have the greatest potential for developing drugs to treat or eradicate these diseases.
原生动物寄生虫病在全球范围内导致了严重的死亡率和发病率。气候变化、极端贫困、移民以及缺乏生活机会等因素导致了被归类为热带病或非地方性疾病的传播。尽管有几种药物可用于对抗寄生虫病,但已报道了对常用药物耐药的菌株。此外,许多一线药物具有从轻度到重度的不良反应,包括潜在的致癌作用。因此,需要新的先导化合物来对抗这些寄生虫。尽管关于低等真核生物的表观遗传机制研究较少,但人们认为表观遗传学在生物体的重要方面起着至关重要的作用,从控制生命周期到参与致病性的基因表达。因此,利用表观遗传靶点对抗这些寄生虫被认为是一个具有巨大发展潜力的领域。本综述总结了主要的已知表观遗传机制及其作为一组医学上重要的原生动物寄生虫治疗方法的潜力。讨论了不同的表观遗传机制,重点介绍了可用于药物重新定位的机制,如组蛋白翻译后修饰(HPTMs)。还强调了独特的寄生虫靶点,包括碱基J和DNA 6 mA。这两类靶点在开发治疗或根除这些疾病的药物方面具有最大的潜力。