Nick-containing oligonucleotides as human topoisomerase I inhibitors

作者：Chua Sock Teng; Quek Ngee Mien^*; Li Ming; Ng Magdeline Tao Tao; Yuan Weixing; Chua May Ling; Guo Juanjuan; Koh Li Eng; Ye Ruijuan; Li Tianhu

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(3): 618-623.

DOI：10.1016/j.bmcl.2008.12.061

• Human topoisomerase I
• Enzyme inhibitor
• Stable hairpins
• Nick oligonucleotides

A series of oligonucleotides with various lengths that contain nick and topoisomerase I-binding sites were designed. The interactions between these oligonucleotides and human topoisomerase I were investigated and the most efficient one among them has displayed IC(50) value of 6.3 nM. Our studies have also demonstrated that the position of the nick as well as the length of the oligonucleotides were crucial factors for the inhibition of this nuclear enzyme.

• 出版日期2009-2-1
• 单位南阳理工学院