Experimental Therapeutics Centre, A*STAR, 31 Biopolis Way, Nanos L3-01, Singapore, 138669, Singapore.
Curr Opin Chem Biol. 2011 Aug;15(4):570-5. doi: 10.1016/j.cbpa.2011.06.016. Epub 2011 Jul 18.
Drug target deconvolution is a process where the action of a drug, a small molecule, is characterised by identifying the proteins binding the drug and initiating the biological effect. The biological relevant target has to be extracted, or deconvoluted, from a list of proteins identified in such an approach. Beside the medically desired action of the drug, the identification of other proteins binding the drug can help to identify side effects and toxicity at a very early stage of drug development. The current approach to identify the proteins binding to the drug is an affinity-enrichment based approach, where the drug molecule is immobilised to a matrix through a linker and the proteins binding to the drug are identified by proteomics.
药物靶点解析是一种通过鉴定与药物结合并引发生物学效应的蛋白质来描述药物(小分子)作用的过程。必须从这种方法中鉴定出的蛋白质列表中提取或解析出生物学相关的靶点。除了药物的医学预期作用外,鉴定与药物结合的其他蛋白质可以帮助在药物开发的早期阶段识别副作用和毒性。目前,鉴定与药物结合的蛋白质的方法是基于亲和富集的方法,其中药物分子通过连接子固定在基质上,通过蛋白质组学鉴定与药物结合的蛋白质。