Energetics of Quadruplex-Drug Recognition in Anticancer Therapy

Author(s): B. Pagano, C. Giancola

Journal Name: Current Cancer Drug Targets

Volume 7 , Issue 6 , 2007

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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

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Article Details

VOLUME: 7
ISSUE: 6
Year: 2007
Page: [520 - 540]
Pages: 21
DOI: 10.2174/156800907781662257
Price: $65

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