Arola Anna, Vilar Ramón
Department of Chemistry, Imperial College London, London SW7 2AZ, United Kingdom.
Curr Top Med Chem. 2008;8(15):1405-15. doi: 10.2174/156802608786141106.
Guanine-rich sequences of DNA can form quadruply-stranded structures. It has been shown that folding single-stranded telomeric DNA into a quadruplex structure inhibits telomerase (an enzyme overexpressed in 85-90% of cancer cells). On the other hand, it has been hypothesised that the formation of quadruplex DNA structures in the promoter region of some oncogenes plays an important role in regulating the transcription of the corresponding gene. Consequently, there is great current interest in developing small molecules that can bind selectively to quadruplex DNA and in doing so could act as anticancer drugs. This review aims to discuss the different types of ligands that have been recently developed as quadruplex DNA stabilisers. The review is organised by the type of compound and mainly covers the literature between 2004 and 2007.
富含鸟嘌呤的DNA序列可形成四链结构。研究表明,将单链端粒DNA折叠成四链结构可抑制端粒酶(一种在85% - 90%的癌细胞中过度表达的酶)。另一方面,有人推测某些癌基因启动子区域四链DNA结构的形成在调节相应基因的转录中起重要作用。因此,目前人们对开发能够选择性结合四链DNA并因此可作为抗癌药物的小分子有着浓厚兴趣。本综述旨在讨论最近作为四链DNA稳定剂开发的不同类型配体。综述按化合物类型编排,主要涵盖2004年至2007年的文献。