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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

A Step Towards Excellence
Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Mechanistic Approach Of Topoisomerase Ii ? Inhibitors For Anticancer Activity: A Review

Author: JEESON BABY, AJAY EMMANUEL THOMAS, ARYA SASANKAN, MRS.SWATHY LEKSHMI, DR.PRASANTH FRANCIS, MR.MANU JOSE
Abstract: DNA topoisomerases are able to solve topological problems resulting from replication, transcription, recombination, and reorganization of the chromatin. Topoisomerases change the state of supercoiling of the DNA and therefore, have great impact on gene activity. The topoisomerases act by transiently cutting one or both strands of the DNA. Type II topoisomerase can relax supercoiled DNA by causing double-stranded break in an ATP and Mg2+ dependent manner. Drugs like Etoposide, Doxorubicin, and Mitoxantrone inhibits both the isoforms of Top II (a and ß) and are regarded as most effective anticancer drugs. Despite the wide applications of topo II inhibitors in cancer therapy, there is still an urgent need to upgrade topo II inhibitors to cope with drug resistance and dose limiting cardiotoxicity. This review focuses on the reported Topoisomerase II a inhibitors in literature and try to analyse the interaction of these molecules with enzyme. Additionally, this study attempts to recognize the common structure features of Top II a inhibitors and correlate it with their reported effects on cell mechanisms and discuss the possibilities of developing specific novel inhibitors.
Keyword: Topoisomerases, Topoisomerase IIa inhibitors, Anticancer agents
DOI: https://doi.org/10.31838/ijpr/2022.14.02.003
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