谷胱甘肽S转移酶的研究进展及其与肿瘤的相关性

药物代谢是细胞解毒机制的重要组成部分之一,其中主要涉及两种酶:Ⅰ和Ⅱ相药物代谢酶。谷胱甘肽S转移酶(GST)是一种重要的Ⅱ相药物代谢酶,可与Ⅰ相药物代谢酶一起催化药物形成高水溶性终产物。所以,GST能够抵御内源性和外源性亲电子物质的损害,并在抗肿瘤过程中发挥重要作用。编码GST的基因至少分布在7条染色体上,构成了一个超基因家族,编码具有GST活性的蛋白。GST有许多功能,传统观点认为,细胞中的GST可发挥防御内、外源性毒性化合物损害的作用。另外,GST在肿瘤细胞中高表达,可介导谷胱甘肽结合至大量抗癌药物底物上,导致肿瘤耐药的发生。

Progress of studies on glutathione-S-transferase and its correlation with tumor

Drug metabolism is one of the most important components in cell detoxification,and two enzymes,i.e.phase Ⅰ drug metabolism enzyme and phase Ⅱ drug metabolism enzyme,are involved in the process.Glutathione-S-transferase(GST) is an important phase Ⅱ drug metabolic enzyme,which,together with phase Ⅰ drug metabolic enzyme,may catalyze drugs to form high water-soluble products.Therefore,GST may counteract the lesions caused by endogenous and exogenous electrophilic substances,and play an important role in antitumorigenisis.The genes coding proteins that have GST activity constitute a super family,and distribute in at least 7 chromosomes.GST possesses many functions,and it is traditionally held that GST may counteract the lesions caused by endogenous and exogenous toxic compounds.Moreover,the over-expression of GST in tumor cells may mediate glutathione to bind on the substrates of anticancer drugs,accordingly leads to drug resistance of tumor.