Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, University of Melbourne, 30 Flemington Rd, Parkville, Victoria 3010, Australia.
Wellcome Trust Centre for Molecular Parasitology, Institute of Infection, Immunity and Inflammation, and Glasgow Polyomics, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8TA, UK.
Parasitology. 2014 Jan;141(1):83-92. doi: 10.1017/S0031182013000814. Epub 2013 Jun 5.
The discovery, development and optimal utilization of pharmaceuticals can be greatly enhanced by knowledge of their modes of action. However, many drugs currently on the market act by unknown mechanisms. Untargeted metabolomics offers the potential to discover modes of action for drugs that perturb cellular metabolism. Development of high resolution LC-MS methods and improved data analysis software now allows rapid detection of drug-induced changes to cellular metabolism in an untargeted manner. Several studies have demonstrated the ability of untargeted metabolomics to provide unbiased target discovery for antimicrobial drugs, in particular for antiprotozoal agents. Furthermore, the utilization of targeted metabolomics techniques has enabled validation of existing hypotheses regarding antiprotozoal drug mechanisms. Metabolomics approaches are likely to assist with optimization of new drug candidates by identification of drug targets, and by allowing detailed characterization of modes of action and resistance of existing and novel antiprotozoal drugs.
通过了解药物的作用模式,可以极大地促进药物的发现、开发和优化利用。然而,目前市场上许多药物的作用机制尚不清楚。非靶向代谢组学有可能发现扰乱细胞代谢的药物的作用模式。高分辨率 LC-MS 方法的发展和改进的数据分析软件现在允许以非靶向的方式快速检测药物对细胞代谢的诱导变化。有几项研究表明,非靶向代谢组学能够为抗菌药物,特别是抗寄生虫药物提供无偏的靶标发现。此外,靶向代谢组学技术的应用使得验证关于抗寄生虫药物作用机制的现有假说成为可能。通过鉴定药物靶点,以及允许对现有和新型抗寄生虫药物的作用模式和耐药性进行详细表征,代谢组学方法可能有助于优化新药候选物。