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Current Cancer Drug Targets

Editor-in-Chief

ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

Energetics of Quadruplex-Drug Recognition in Anticancer Therapy

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

Volume 7, Issue 6, 2007

Page: [520 - 540] Pages: 21

DOI: 10.2174/156800907781662257

Price: $65

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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