Abstract
Guanine-rich sequences of DNA can form quadruply-stranded structures. It has been shown that folding singlestranded telomeric DNA into a quadruplex structure inhibits telomerase (an enzyme overexpressed in 85-90% of cancer cells). On the other hand, it has been hypothesised that the formation of quadruplex DNA structures in the promoter region of some oncogenes plays an important role in regulating the transcription of the corresponding gene. Consequently, there is great current interest in developing small molecules that can bind selectively to quadruplex DNA and in doing so could act as anticancer drugs. This review aims to discuss the different types of ligands that have been recently developed as quadruplex DNA stabilisers. The review is organised by the type of compound and mainly covers the literature between 2004 and 2007.
Keywords: Quadruplex DNA, telomerase inhibition, oncogene regulation, small molecule
Current Topics in Medicinal Chemistry
Title: Stabilisation of G-Quadruplex DNA by Small Molecules
Volume: 8 Issue: 15
Author(s): Anna Arola and Ramon Vilar
Affiliation:
Keywords: Quadruplex DNA, telomerase inhibition, oncogene regulation, small molecule
Abstract: Guanine-rich sequences of DNA can form quadruply-stranded structures. It has been shown that folding singlestranded telomeric DNA into a quadruplex structure inhibits telomerase (an enzyme overexpressed in 85-90% of cancer cells). On the other hand, it has been hypothesised that the formation of quadruplex DNA structures in the promoter region of some oncogenes plays an important role in regulating the transcription of the corresponding gene. Consequently, there is great current interest in developing small molecules that can bind selectively to quadruplex DNA and in doing so could act as anticancer drugs. This review aims to discuss the different types of ligands that have been recently developed as quadruplex DNA stabilisers. The review is organised by the type of compound and mainly covers the literature between 2004 and 2007.
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Cite this article as:
Arola Anna and Vilar Ramon, Stabilisation of G-Quadruplex DNA by Small Molecules, Current Topics in Medicinal Chemistry 2008; 8 (15) . https://dx.doi.org/10.2174/156802608786141106
DOI https://dx.doi.org/10.2174/156802608786141106 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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