Development of DNA Topoisomerase-Related Therapeutics: A Short Perspective of New Challenges

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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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Development of DNA Topoisomerase-Related Therapeutics: A Short Perspective of New Challenges

Anti-Cancer Agents in Medicinal Chemistry, 4(4): 335-345.

Author(s): Giovanni Capranico, Giuseppe Zagotto and Manlio Palumbo.

Affiliation: Department of Biochemistry “G. Moruzzi”, Alma Mater Studiorum University of Bologna, via Irnerio 48,40126 Bologna, Italy


Antitumor agents targeting DNA and DNA-associated processes are widely used in the treatment of human cancers and produce significant increases in the survival of patients. DNA topoisomerases remain the most significant target of these cytotoxic drugs and constitute a growing family of nuclear enzymes that regulate DNA topology during DNA replication and recombination, DNA transcription, chromosome condensation-decondensation and segregation. Major progress has been attained in recent years in the understanding of the structures of these enzymes and their main cellular functions, hopefully providing new opportunities for pharmacological interventions. New leads and derivatives of known structures have been reported recently, and here they will be discussed highlighting the challenges to find innovative and more effective drugs. Moreover, we will review novel and diverse approaches relevant to the development of new topoisomerase-related therapeutics.


topoisomerase, topoisomerase-directed drugs, crystal structures, protein toxins, drug receptor, cancer.

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Article Details

Volume: 4
Issue Number: 4
First Page: 335
Last Page: 345
Page Count: 11
DOI: 10.2174/1568011043352885
Price: $58

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