Indian Journal of Pharmacy and Pharmacology

Print ISSN: 2393-9079

Online ISSN: 2393-9087

CODEN : IJPPTK

Indian Journal of Pharmacy and Pharmacology (IJPP) open access, peer-reviewed quarterly journal publishing since 2014 and is published under auspices of the Innovative Education and Scientific Research Foundation (IESRF), aim to uplift researchers, scholars, academicians, and professionals in all academic and scientific disciplines. IESRF is dedicated to the transfer of technology and research by publishing scientific journals, research content, providing professional’s membership, and conducting conferences, seminars, and award programs. With more...

Article type

Review Article


Article page

13-17


Authors Details

Suraksha Kadam, Disha Sharma, Manisha Mishra, Vaidhun Bhaskar, Preeti Kulkarni*


Article Metrics


View Article As

 


Downlaod Files

   






Article statistics

Viewed: 421

PDF Downloaded: 358


DNA Topoisomerases: As target for anti-cancer drugs


Review Article

Author Details : Suraksha Kadam, Disha Sharma, Manisha Mishra, Vaidhun Bhaskar, Preeti Kulkarni*

Volume : 9, Issue : 1, Year : 2022

Article Page : 13-17

https://doi.org/10.18231/j.ijpp.2022.003



Suggest article by email

Get Permission

Abstract

Topoisomerase inhibitors are agents designed to interfere with the action of topoisomerase enzymes I and II. Topoisomerases are enzymes that control the changes in DNA tridimensional structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle. DNA Topoisomerases control the conformational changes in DNA topology by breaking and resealing DNA strands during normal cellular growth, that’s why these are essential enzymes. A major class of anticancer drugs acts as inhibitors of DNA Topoisomerases. This paper gives a brief review on Topoisomerase targeting drugs which shows anticancer activities. The mechanism of action of these drugs by inhibiting type I and type II DNA Topoisomerases are discussed. DNA topoisomerases, especially type II A topoisomerases, are proved therapeutic targets of anticancer and antibacterial drugs. Clinically successful topoisomerase-targeting anticancer drugs act through topoisomerase poisoning, which leads to replication fork arrest and double-strand break formation. Unfortunately, this unique mode of action is associated with the development of secondary cancers and cardiotoxicity. Structures of topoisomerase–drug–DNA ternary complexes have revealed the exact binding sites and mechanisms of topoisomerase poisons. It may also be possible to design catalytic inhibitors of topoisomerases by targeting certain inactive conformations of these enzymes. Furthermore, identification of various new bacterial topoisomerase inhibitors and regulatory proteins may inspire the discovery of novel human topoisomerase inhibitors. Thus, topoisomerases remain as important therapeutic targets of anticancer agents.


Keywords: Anticancer Agent, Topoisomerases, Topoisomerase I, Topoisomerase II, topoisomerase poison


How to cite : Kadam S, Sharma D, Mishra M, Bhaskar V, Kulkarni P, DNA Topoisomerases: As target for anti-cancer drugs. Indian J Pharm Pharmacol 2022;9(1):13-17

This is an Open Access (OA) journal, and articles are distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as appropriate credit is given and the new creations are licensed under the identical terms.