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Current Drug Targets


ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

The Genome as a Drug Target Sequence Specific Minor Groove Binding Ligands

Author(s): P. R. Turner and W. A. Denny

Volume 1, Issue 1, 2000

Page: [1 - 14] Pages: 14

DOI: 10.2174/1389450003349407


The ability to target defined sequences on the DNA molecule would be of enormous benefit to the treatment of human disease. Towards this goal much research has been invested in examining the DNA binding and biological mechanisms of action of sequence selective minor groove binding ligands. These compounds act in a variety of ways to inhibit gene expression and DNA replication and also alternuclear architecture. Concomitant with this, minor groove adducts formed by certain compounds are inefficiently removed by cellular DNA repair systems and are extremely cytotoxic. Additionally compounds targeting A.T rich DNA sequences have found clinical use in the treatment of particular parasitic infections.

Keywords: Drug Target Cellular, Minor Groove Binding Ligands, DNA Binding, DNA Gene expression, Parasitic infectious, Cytotoxic, Plasmodium, Falciparum, DNA replication, DNA Alkylating compounds

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