Recognition of forcible curvature in circular DNA by human topoisomerase I

Yang, Zhaoqi; Li, Dawei; Hiew, Shuhui; Ng, Magdeline Taotao; Yuan, Weixing; Su, Haibin; Shao, Fangwei; Li, Tianhu

doi:10.1039/c1cc13904e

Cited by 5 publications

(1 citation statement)

References 28 publications

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“…Further investigations revealed that when gap, nick-containing, C3-spacer-containing, and so on, were constructed into the non-supercoiled substrates, the resultant duplex structures could form covalent linkages with topoisomerase I in irreversible fashions 24–29 . In addition, certain non-supercoiled DNA was designed in our previously studies that displayed high inhibition on the activity of human topoisomerase I according to the recognise characteristic of the enzyme 30–33 . These previous studies have inspired us to speculate that the non-supercoiled oligonucleotides, if modified properly in its structure (such as introduced into a bulge structure), could serve as an inhibitor of Btopo I in the relaxation reaction of supercoiled DNA.…”

Section: Introductionmentioning

confidence: 99%

Bulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I

Yang

Jiang

Zhong

et al. 2017

Journal of Enzyme Inhibition and Medicinal Chemistry

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Bacterial topoisomerase I (Btopo I) was defined as potential target for discovery of new antibacterial compounds. Various oligonucleotides containing bulge structure were designed and synthesised as inhibitors to Btopo I in this investigation. The results of this study demonstrated that the designed oligonucleotides display high inhibitory efficiency on the activity of Btopo I and the inhibitory effect could be modulated by the amount of bulge DNA bases. The most efficient one among them showed an IC50 value of 63.1 nM in its inhibition on the activity of Btopo I. In addition, our studies confirmed that the designed oligonucleotide would induce irreversible damages to Btopo I and without any effects occur to eukaryotic topoisomerase I. It is our hope that the results provided in these studies could provide a novel way to inhibit Btopo I.

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Section: Introductionmentioning

confidence: 99%