National Institute of Malaria Research (ICMR), Sector-8, Dwarka, New Delhi, India.
Department of Biochemistry, North Delhi Municipal Corporation Medical College & Hindu Rao Hospital, Delhi-110007, India.
Curr Top Med Chem. 2018;18(22):1987-1997. doi: 10.2174/1568026619666181130134742.
Malaria continues to impinge heavily on mankind, with five continents still under its clasp. Widespread and rapid emergence of drug resistance in the Plasmodium parasite to current therapies accentuate the quest for novel drug targets and antimalarial compounds. Plasmodium parasites, maintain a non-photosynthetic relict organelle known as Apicoplast. Among the four major pathways of Apicoplast, biosynthesis of isoprenoids via Methylerythritol phosphate (MEP) pathway is the only indispensable function of Apicoplast that occurs during different stages of the malaria parasite. Moreover, the human host lacks MEP pathway. MEP pathway is a validated repertoire of novel antimalarial and antibacterial drug targets. Fosmidomycin, an efficacious antimalarial compound against IspC enzyme of MEP pathway is already in clinical trials as a combination drugs. Exploitation of other enzymes of MEP pathway would provide a much-needed impetus to the antimalarial drug discovery programs for the elimination of malaria. We outline the cardinal features of the MEP pathway enzymes and progress made towards the characterization of new inhibitors.
疟疾继续严重影响人类,五大洲仍深受其害。疟原虫对现有疗法的耐药性广泛而迅速出现,这突显了对新型药物靶点和抗疟化合物的需求。疟原虫寄生虫维持着一种非光合的遗留细胞器,称为质体。在质体的四个主要途径中,通过甲羟戊酸(MEP)途径合成异戊烯醇是质体在疟原虫不同阶段唯一不可缺少的功能。此外,人体宿主缺乏 MEP 途径。MEP 途径是一种经过验证的新型抗疟和抗菌药物靶点。福米霉素是一种针对 MEP 途径的 IspC 酶的有效抗疟化合物,已作为组合药物进入临床试验。利用 MEP 途径的其他酶将为消除疟疾的抗疟药物发现计划提供急需的推动力。我们概述了 MEP 途径酶的主要特征,并介绍了针对新型抑制剂的表征所取得的进展。