DNA Topoisomerases as Anticancer Drug Targets: From the Laboratory to the Clinic

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 17, 14 Issues, 2017


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

This journal supports open access

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
ICCF-CNRS UMR 6296
Université Clermont Auvergne
Clermont-Ferrand
France


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

DNA Topoisomerases as Anticancer Drug Targets: From the Laboratory to the Clinic



Anti-Cancer Agents in Medicinal Chemistry, 1(1): 1-25.

Author(s): Joseph A Holden.

Affiliation: Department of Pathology, University of Utah, Salt Lake City, Utah, 84132, USA.

Abstract

DNA topoisomerases play important roles in basic cellular biology. Recently they have been identified as the molecular targets of a variety of pharmaceutical agents. Some of the drugs that target the topoisomerases are anticancer drugs. These anticancer drugs work by a novel mechanism of action. They inhibit the topoisomerase molecule from religating DNA strands after cleavage. This leaves a cell with DNA breaks, which if not repaired, become lethal. In other words, these drugs convert the topoisomerase molecule into a DNA damaging agent. This is a stoichiometric relationship. Each anticancer drug molecule has the potential of interacting with one topoisomerase molecule to cause one DNA lesion. The clinical implication of this mechanism of drug action is that sensitivity to topoisomerase targeting drugs should be dependent on high topoisomerase levels. This is clearly true in laboratory systems. With new developments in in situ immunohistochemistry, topoisomerase expression can now be easily estimated in human cancers. From this information, it may be possible to predict the sensitivity or resistance of human cancers to topoisomerase targeting anticancer drugs.

Keywords:

DNA Topoisomerases, Anticancer Drug Targets, cleavable complex, heterotetramer, Eukaryotic, BLM gene, terminal arms, Camptotheca acuminata, Topotecan and Irinotecan, mitoxantrone.



Download Free Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 1
Issue Number: 1
First Page: 1
Last Page: 25
Page Count: 25
DOI: 10.2174/1568011013354859
Advertisement
Global Biotechnology Congress 2017Drug Discovery and Therapy World Congress 2017

Related Journals




Related eBooks



Webmaster Contact: urooj@benthamscience.org Copyright © 2017 Bentham Science