Please use this identifier to cite or link to this item: http://lib.jncasr.ac.in:8080/jspui/handle/10572/2599
Title: Inhibition of Mycobacterium tuberculosis topoisomerase I by m-AMSA, a eukaryotic type II topoisomerase poison
Authors: Godbole, Adwait Anand
Ahmed, Wareed
Bhat, Rajeshwari Subray
Bradley, Erin K.
Ekins, Sean
Nagaraja, V.
Keywords: Biochemistry & Molecular Biology
Biophysics
M-Amsa
Type I Topoisomerase
Mycobacterium Tuberculosis
Topoisomerase Inhibitors
DNA Topoisomerases
Anticancer Drugs
Cleavage
Mechanism
Gyrase
Complex
Enzyme
Religation
Amsacrine
Leukemia
Issue Date: 2014
Publisher: Academic Press Inc Elsevier Science
Citation: Godbole, AA; Ahmed, W; Bhat, RS; Bradley, EK; Ekins, S; Nagaraja, V, Inhibition of Mycobacterium tuberculosis topoisomerase I by m-AMSA, a eukaryotic type II topoisomerase poison. Biochemical And Biophysical Research Communications 2014, 446 (4) 916-920, http://dx.doi.org/10.1016/j.bbrc.2014.03.029
Biochemical And Biophysical Research Communications
446
4
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.
Description: Restricted Access
URI: http://hdl.handle.net/10572/2599
ISSN: 0006-291X
Appears in Collections:Research Articles (Nagaraja, V.)

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