近年研究表明,G一四链体在原癌基因启动子、端粒DNA和信使RNA非编码区均过度表达,寻找能够稳定或诱导这些G.四链体的配体分子,继而抑制基因的转录及相关蛋白的翻译过程,将会发展成为一种新型的抗癌策略。本文对G一四链体结构数据库及以此为靶点的抗癌机制和小分子配体研究进展进行综述。
In recent years, Gquadruplexes overexpression has been found in different biologically significant regions, such as oncogenepromoter regions, human telomeres DNA and mRNA 5'untranslated region (UTR). Therefore, a novel anticancer strategy may be developed by searching some ligands to stabilize or to induce the Gquadruplexs so as to inhibit cancer gene transcription and translation process. The current structural database of folding topologies, the anticancer mechanism targeting different types of G quadruplex, and the progresses on the corresponding small molecular ligands as potent antitumor agents are summarized in this re