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Recent Developments in the Chemistry and Biology of G-Quadruplexes with Reference to the DNA Groove Binders

Jain, Akash K and Bhattacharya, Santanu (2012) Recent Developments in the Chemistry and Biology of G-Quadruplexes with Reference to the DNA Groove Binders. In: CURRENT PHARMACEUTICAL DESIGN, 18 (14). pp. 1917-1933.

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Abstract

DNA is the chemotherapeutic target for treating diseases of genetic origin. Besides well-known double-helical structures (A, B, Z, parallel stranded-DNA etc.), DNA is capable of forming several multi-stranded structures (triplex, tetraplex, i-motif etc.) which have unique biological significance. The G-rich 3'-ends of chromosomes, called telomeres, are synthesized by telomerase, a ribonucleoprotein, and over-expression of telomerase is associated with cancer. The activity of telomerase is suppressed if the G-rich region is folded into the four stranded structures, called G-quadruplexes (G4-DNAs) using small synthetic ligands. Thus design and synthesis of new G4-DNA ligands is an attractive strategy to combat cancer. G4-DNA forming sequences are also prevalent in other genomic regions of biological significance including promoter regions of several oncogenes. Effective gene regulation may be achieved by inducing a G4-DNA structure within the G-rich promoter sequences. To date, several G4-DNA stabilizing ligands are known. DNA groove binders interact with the duplex B-DNA through the grooves (major and minor groove) in a sequence-specific manner. Some of the groove binders are known to stabilize the G4-DNA. However, this is a relatively under explored field of research. In this review, we focus on the recent advances in the understanding of the G4-DNA structures, particularly made from the human telomeric DNA stretches. We summarize the results of various investigations of the interaction of various organic ligands with the G4-DNA while highlighting the importance of groove binder-G4-DNA interactions.

Item Type: Journal Article
Keywords: Telomere;telomerase;G-quadruplex;G-quadruplex ligands;groove binding ligands
Department/Centre: Division of Chemical Sciences > Organic Chemistry
Date Deposited: 06 Jul 2012 12:38
Last Modified: 06 Jul 2012 12:39
URI: http://eprints.iisc.ernet.in/id/eprint/44770

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