Avitia-Domínguez Claudia, Sierra-Campos Erick, Betancourt-Conde Irene, Aguirre-Raudry Miriam, Vázquez-Raygoza Alejandra, Luevano-De la Cruz Artemisa, Favela-Candia Alejandro, Sarabia-Sanchez Marie, Ríos-Soto Lluvia, Méndez-Hernández Edna, Cisneros-Martínez Jorge, Palacio-Gastélum Marcelo Gómez, Valdez-Solana Mónica, Hernández-Rivera Jessica, De Lira-Sánchez Jaime, Campos-Almazán Mara, Téllez-Valencia Alfredo
Facultad de Medicina y Nutrición, Universidad Juárez del Estado de Durango, Av. Universidad y Fanny Anitua S/N, Durango. Dgo. México, C.P. 34000.
Curr Protein Pept Sci. 2016;17(3):260-74. doi: 10.2174/1389203717999160226180353.
Malaria is one of the main infectious diseases in tropical developing countries and represents high morbidity and mortality rates nowadays. The principal etiological agent P. falciparum is transmitted through the bite of the female Anopheles mosquito. The issue has escalated due to the emergence of resistant strains to most of the antimalarials used for the treatment including Chloroquine, Sulfadoxine-Pyrimethamine, and recently Artemisinin derivatives, which has led to diminished effectiveness and by consequence increased the severity of epidemic outbreaks. Due to the lack of effective compounds to treat these drug-resistant strains, the discovery or development of novel anti-malaria drugs is important. In this context, one strategy has been to find inhibitors of enzymes, which play an important role for parasite survival. Today, promising results have been obtained in this regard, involving the entire P. falciparum metabolism. These inhibitors could serve as leads in the search of a new chemotherapy against malaria. This review focuses on the achievements in recent years with regard to inhibition of enzymes used as targets for drug design against malaria.
疟疾是热带发展中国家的主要传染病之一,目前发病率和死亡率都很高。主要病原体恶性疟原虫通过雌性按蚊叮咬传播。由于对包括氯喹、磺胺多辛-乙胺嘧啶以及最近的青蒿素衍生物在内的大多数用于治疗的抗疟药物出现了耐药菌株,这个问题已经升级,这导致疗效降低,进而增加了疫情爆发的严重程度。由于缺乏治疗这些耐药菌株的有效化合物,发现或开发新型抗疟药物很重要。在这种背景下,一种策略是寻找对寄生虫生存起重要作用的酶的抑制剂。如今,在这方面已经取得了有前景的成果,涉及恶性疟原虫的整个新陈代谢。这些抑制剂可以作为寻找抗疟疾新化疗方法的先导。这篇综述聚焦于近年来在抑制用作抗疟疾药物设计靶点的酶方面所取得的成果。