摘要
乙二醛酶(Glyoxalase,GLO)Ⅰ抑制剂是以GLOⅠ为靶点的一类药物,它能通过抑制肿瘤细胞中的GLOⅠ,使GLO底物甲基乙二醛(methylglyoxal MG)在肿瘤细胞中达到毒性浓度,产生抑制肿瘤生长和逆转肿瘤耐药的作用。随着GLOⅠ抑制剂家族成员数量的不断增加,其抗癌范围也在不断扩大。本综述对GLOⅠ抑制剂抗肿瘤原理及逆转耐药机理的研究现状进行阐述,并对近几年出现的GLOⅠ抑制剂,主要是以谷胱甘肽为基本结构和天然化合物类的GLOⅠ抑制剂进行总结,希望对GLOⅠ抑制剂的研发和应用起到一定的促进作用。
ABSTRACT Glyoxalase （GLO） Ⅰ inhibitor is a class of antitumor agents that target GLO Ⅰ. It can inhibit tumor growth and reverse the anticancer drug resistance by inhibiting GLO I to make methylglyoxal （MG） accumulate to toxicity level in tumor cells. As an important direction of cancer treatment,GLO I inhibitor has become a hot topic on anti-tumor drug for its great performance in antitumor efficacy and is attracting more and more attention from home and abroad. As a result, many related compounds have been developed, members of GLO I inhibitors are ever-increasing and their anti-cancer spectra are also expanding. With the improvement of technology, their anti-tumor principle and their mechanism in reversal of anticancer drug resistance are also being studied deeply, which suggest that the agents of this group could not only be used alone. It would be more effective if combining with other antitumor drugs on clinical in the future. This review aims to describe the developments of members in this family, especially the natural compounds of GLO Ⅰ inhibitors and those compounds based on glutathione （GSH）. The progress of GLO Ⅰ inhibitors on their anti-tumor principle and their mechanism of the reversal of anticancer drug resistance are also mentioned here. It is hoped that this article would be a promotion to the development of GLO Ⅰ inhibitors as well as to the research of anticancer agents.
出处
《药学与临床研究》
2011年第4期337-342,共6页
Pharmaceutical and Clinical Research
