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Inhibition of Mycobacterium tuberculosis topoisomerase I by m-AMSA, a eukaryotic type II topoisomerase poison

Godbole, Adwait Anand and Ahmed, Wareed and Bhat, Rajeshwari Subray and Bradley, Erin K and Ekins, Sean and Nagaraja, Valakunja (2014) Inhibition of Mycobacterium tuberculosis topoisomerase I by m-AMSA, a eukaryotic type II topoisomerase poison. In: BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 446 (4). pp. 916-920.

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Official URL: http://dx.doi.org/10.1016/j.bbrc.2014.03.029

Abstract

m-AMSA, an established inhibitor of eukaryotic type II topoisomerases, exerts its cidal effect by binding to the enzyme-DNA complex thus inhibiting the DNA religation step. The molecule and its analogues have been successfully used as chemotherapeutic agents against different forms of cancer. After virtual screening using a homology model of the Mycobacterium tuberculosis topoisomerase I, we identified m-AMSA as a high scoring hit. We demonstrate that m-AMSA can inhibit the DNA relaxation activity of topoisomerase I from M. tuberculosis and Mycobacterium smegmatis. In a whole cell assay, m-AMSA inhibited the growth of both the mycobacteria. (C) 2014 Elsevier Inc. All rights reserved.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to the ACADEMIC PRESS INC ELSEVIER SCIENCE, USA
Keywords: m-AMSA; Type I topoisomerase; Mycobacterium tuberculosis; Topoisomerase inhibitors
Department/Centre: Division of Biological Sciences > Microbiology & Cell Biology
Depositing User: Id for Latest eprints
Date Deposited: 11 Jun 2014 10:30
Last Modified: 11 Jun 2014 10:30
URI: http://eprints.iisc.ac.in/id/eprint/49177

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