Quadruplex-Duplex Motifs as New Topoisomerase I Inhibitors |
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| Authors: | Li Shuai Minggang Deng Dan Zhang Yangyang Zhou Xiang Zhou |
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| Affiliation: | 1. College of Pharmacy , South-Central University for Nationalities , Hubei, Wuhan, P. R. China;2. State Key Laboratory of Virology, Department of Immunology , Wuhan University School of Medicine , Hubei, Wuhan, P. R. China;3. College of Chemitry and Molecular Sciences , Wuhan University , Hubei, Wuhan, P. R. China |
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| Abstract: | In this article, 13 short chains that can form G-quadruplex and quadruplex-duplex motif have been designed. Fourteen oligonucleotides, including 13 short chains as well as a reference short chain all have certain level of inhibition to topoisomerase I, whether or not they form G-quadruplex and quadruplex-duplex motif, and the G-quadruplex and quadruplex-duplex motif show better activity than single short chain. The result confirmed that after forming G-quadruplex and quadruplex-duplex motif these 14 oligonucleotides are competitive inhibition, that is, through the priority binding with the topoisomerase I and precluding from its binding with the normal substrate pBR322 and, therefore, inhibiting the next reaction. |
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| Keywords: | Topoisomerase I G-quadruplex quadruplex-duplex motif |
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