Therapeutic Agents Based on DNA Sequence Specific Binding

Author(s): Luke Pett, John A. Hartley, Konstantinos Kiakos

Journal Name: Current Topics in Medicinal Chemistry

Volume 15 , Issue 14 , 2015

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Graphical Abstract:


DNA interactive agents have been used in the clinical setting for the treatment of cancer since the beginning of modern-era chemotherapy. Despite a shift of focus towards molecular targeted therapy, DNA remains a critical macromolecular target for anti-cancer intervention and the next generation of agents must conform to the optimum combination of increased therapeutic activity and reduced off-target toxicity. We evaluate the potential of non-covalent DNA binding small molecules as “gene-control” agents, exploiting inherent or engineered sequence selectivity, to target critical genomic sequences. In addition we review examples of natural products and synthetic derivatives that exert their activity through sequence specific DNA-covalent modification.

Keywords: Alkylating agents, Anticancer chemotherapeutics, Covalent binding, DNA recognition, DNA-targeting agents, Non-covalent binding, Polyamides, Sequence specificity.

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Article Details

Year: 2015
Page: [1293 - 1322]
Pages: 30
DOI: 10.2174/1568026615666150413155431
Price: $65

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PDF: 59