Quadruplex-duplex motifs as new topoisomerase I inhibitors.
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.
College of Pharmacy, South-Central University for Nationalities, Hubei, Wuhan, P. R. China. shuaich@163.com
Li
L
Shuai
Minggang
M
Deng
Dan
D
Zhang
Yangyang
Y
Zhou
Xiang
X
Zhou
D001483:Base Sequence; D002942:Circular Dichroism; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D024202:Electrophoretic Mobility Shift Assay; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D054856:G-Quadruplexes; D008969:Molecular Sequence Data; D009690:Nucleic Acid Conformation; D009841:Oligonucleotides / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D009841:Oligonucleotides; D004264:DNA Topoisomerases, Type I