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

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


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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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.



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Article Details

Volume: 1
Issue Number: 1
First Page: 1
Last Page: 25
Page Count: 25
DOI: 10.2174/1568011013354859
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