Therapeutic Agents Based on DNA Sequence Specific Binding

Title:Therapeutic Agents Based on DNA Sequence Specific Binding

Volume: 15 Issue: 14

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

Affiliation:

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

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.

Cite this article as:

Pett Luke, A. Hartley John and Kiakos Konstantinos, Therapeutic Agents Based on DNA Sequence Specific Binding, Current Topics in Medicinal Chemistry 2015; 15(14) . https://dx.doi.org/10.2174/1568026615666150413155431