Abstract
Immortality of tumour cells is strictly correlated to telomerase activity. Telomerase is overexpressed in about 85% of tumour cells and maintains telomere length contributing to cell immortalisation, whereas in somatic cells telomeres progressively shorten until cell death occurs by apoptosis. Different drugs can promote telomeric G-rich overhangs which fold into quadruplex structures that inhibit telomerase activity. Detailed studies on drug-quadruplex complexes are essential to understand quadruplex recognition and address drug design. This review will discuss the energetic aspects of quadruplex-drug interactions with a particular attention to physico-chemical methodologies.
Keywords: Telomerase, telomeric DNA, G-quadruplex, G-quadruplex-drug interactions, physico-chemical techniques
Current Cancer Drug Targets
Title: Energetics of Quadruplex-Drug Recognition in Anticancer Therapy
Volume: 7 Issue: 6
Author(s): B. Pagano and C. Giancola
Affiliation:
Keywords: Telomerase, telomeric DNA, G-quadruplex, G-quadruplex-drug interactions, physico-chemical techniques
Abstract: Immortality of tumour cells is strictly correlated to telomerase activity. Telomerase is overexpressed in about 85% of tumour cells and maintains telomere length contributing to cell immortalisation, whereas in somatic cells telomeres progressively shorten until cell death occurs by apoptosis. Different drugs can promote telomeric G-rich overhangs which fold into quadruplex structures that inhibit telomerase activity. Detailed studies on drug-quadruplex complexes are essential to understand quadruplex recognition and address drug design. This review will discuss the energetic aspects of quadruplex-drug interactions with a particular attention to physico-chemical methodologies.
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Cite this article as:
Pagano B. and Giancola C., Energetics of Quadruplex-Drug Recognition in Anticancer Therapy, Current Cancer Drug Targets 2007; 7 (6) . https://dx.doi.org/10.2174/156800907781662257
DOI https://dx.doi.org/10.2174/156800907781662257 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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