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Bulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I.

ABSTRACT: 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.

SUBMITTER: Yang Z

PROVIDER: S-EPMC6009931 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

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Bulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I.

Yang Zhaoqi Z Jiang Tuoyu T Zhong Hanshi H Kang Yu Y

Journal of enzyme inhibition and medicinal chemistry 20181201 1

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 ...[more]

PMID: 29281935

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