Energetics of quadruplex-drug recognition in anticancer therapy |
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Authors: | Pagano B Giancola C |
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Institution: | Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy. |
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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. |
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