Vázquez Karina, Paulino Margot, Salas Cristian O, Zarate-Ramos Juan J, Vera Brenda, Rivera Gildardo
Facultad de Medicina Veterinaria y Zootecnia, Universidad Autónoma de Nuevo León, Escobedo, 66050, Mexico.
Centro de Bioinformática Estructural DETEMA, Facultad de Química, Universidad de la Republica, P.O. 1157, Montevideo, Uruguay.
Mini Rev Med Chem. 2017;17(11):939-946. doi: 10.2174/1389557517666170315145410.
BACKGROUND & OBJECTIVE: Chagas disease or American trypanosomiasis is a major parasitic disease in Latin America with restricted available treatment: nifurtimox and benznidazole. These two drugs are ineffective in the chronic phase of the disease; therefore, there is a need for the development of new, efficient and safe drugs for the treatment of this pathology. With this goal, one of the promising targets is trypanothione reductase (TR), a key enzyme in the metabolism of Trypanosoma cruzi.
In this review, we analyse the importance of TR as a drug target, as well as the well-known and new inhibitors reported in the last decade as potential therapeutic agents for Chagas disease.
恰加斯病或美洲锥虫病是拉丁美洲一种主要的寄生虫病，可用治疗方法有限：硝呋莫司和苯硝唑。这两种药物在该病的慢性期无效；因此，需要研发新的、高效且安全的药物来治疗这种病症。出于这一目标，一个有前景的靶点是锥虫硫醇还原酶（TR），它是克氏锥虫代谢中的关键酶。
在本综述中，我们分析了TR作为药物靶点的重要性，以及过去十年报道的作为恰加斯病潜在治疗药物的知名抑制剂和新抑制剂。
