Khan Sameena
Drug Discovery Research Centre, Translational Health Science and Technology Institute (THSTI), NCR Biotech Science Cluster, 3rd Milestone, Faridabad-Gurgaon Expressway, PO box #04, Faridabad, 121001, India.
Malar J. 2016 Apr 12;15:203. doi: 10.1186/s12936-016-1247-0.
Escalating drug resistance in malaria parasites and lack of vaccine entails the discovery of novel drug targets and inhibitor molecules. The multi-component protein translation machinery is a rich source of such drug targets. Malaria parasites contain three translational compartments: the cytoplasm, apicoplast and mitochondrion, of which the latter two are of the prokaryotic type. Recent explorations by many groups into the malaria parasite protein translation enzymes, aminoacyl-tRNA synthetases (aaRSs), have yielded many promising inhibitors. The understanding of the biology of this unique set of 36 enzymes has become much clearer in recent times. Current review discusses the advances made in understanding of crucial aaRSs from Plasmodium and also the specific inhibitors found against malaria aaRSs.
疟原虫耐药性不断升级且缺乏疫苗,这就需要发现新的药物靶点和抑制剂分子。多组分蛋白质翻译机制就是这类药物靶点的丰富来源。疟原虫含有三个翻译区室:细胞质、顶质体和线粒体,其中后两者属于原核类型。最近许多研究小组对疟原虫蛋白质翻译酶——氨酰-tRNA合成酶(aaRSs)进行了探索,已产生了许多有前景的抑制剂。近年来,对这组独特的36种酶的生物学特性的了解已变得更加清晰。本综述讨论了在了解疟原虫关键氨酰-tRNA合成酶方面取得的进展,以及针对疟原虫氨酰-tRNA合成酶发现的特异性抑制剂。