Generic placeholder image

Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Therapeutic Agents Based on DNA Sequence Specific Binding

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

Volume 15, Issue 14, 2015

Page: [1293 - 1322] Pages: 30

DOI: 10.2174/1568026615666150413155431

Price: $65


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.

Graphical Abstract

Rights & Permissions Print Export Cite as
© 2023 Bentham Science Publishers | Privacy Policy