Energetics of quadruplex-drug recognition in anticancer therapy

Curr Cancer Drug Targets. 2007 Sep;7(6):520-40. doi: 10.2174/156800907781662257.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Humans
  • Telomerase / metabolism*
  • Telomere

Substances

  • Antineoplastic Agents
  • Telomerase