Thanna Sandeep, Sucheck Steven J
Department of Chemistry and Biochemistry, The University of Toledo, 2801 W. Bancroft Street, MS602, Toledo, OH, USA 43606.
Medchemcomm. 2016;7(1):69-85. doi: 10.1039/C5MD00376H. Epub 2015 Oct 16.
Tuberculosis (TB) is an epidemic disease and the growing burden of multidrug-resistant (MDR) TB world wide underlines the need to discover new drugs to treat the disease. () is the etiological agent of most cases of TB. is difficult to treat, in part, due to the presence of a sturdy hydrophobic barrier that prevents penetration of drugs through the cell wall. can also survive in a non-replicative state for long periods of time avoiding the action of common antibiotics. Trehalose is an essential metabolite in mycobacteria since it plays key roles in cell wall synthesis, transport of cell wall glycolipids, and energy storage. It is also known for its stress protective roles such as: protection from desiccation, freezing, starvation and osmotic stress in bacteria. In this review we discuss the drug discovery efforts against enzymes involved in the trehalose utilization pathways (TUPs) and their likelihood of becoming drug targets.
结核病(TB)是一种流行病,全球耐多药(MDR)结核病负担日益加重,这凸显了研发新药物治疗该病的必要性。()是大多数结核病病例的病原体。()难以治疗,部分原因是存在坚固的疏水屏障,阻止药物穿透细胞壁。()还可以长时间处于非复制状态存活,从而避免普通抗生素的作用。海藻糖是分枝杆菌中的一种必需代谢物,因为它在细胞壁合成、细胞壁糖脂运输和能量储存中起关键作用。它还因其应激保护作用而闻名,例如:保护细菌免受干燥、冷冻、饥饿和渗透应激。在本综述中,我们讨论了针对海藻糖利用途径(TUPs)中相关酶的药物研发工作以及它们成为药物靶点的可能性。
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