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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Searching Drug-Like Anti-cancer Compound(s) Based on G-Quadruplex Ligands

Author(s): Qian Li, Jun-Feng Xiang, Hong Zhang and Ya-Lin Tang

Volume 18, Issue 14, 2012

Page: [1973 - 1983] Pages: 11

DOI: 10.2174/138161212799958369

Price: $65

Abstract

G-quadruplex structure is a four-stranded form of DNA, which is associated with cancer cell proliferation. G-quadruplexstabilized ligands have the potential to interfere with telomere replication by blocking the elongation procedure catalyzed by telomerase, and therefore have the potential to be anti-cancer drugs. A considerable number of novel compounds capable of targeting G-quadruplex at high affinity and specificity have been reported. Among them, several G-quadruplex ligands have shown promising anti-cancer activity in tumor xenograft models, and entered phase II clinical trials on cancer patients. This review summarized recent developments of Gquadruplex ligands as anti-cancer drugs and several powerful strategies to discover novel G-quadruplex ligands as anti-cancer drug candidates by screening natural product extracts and structural optimization of previously identified typical compounds.

Keywords: G-quadruplex, anti-cancer, drug screening, drug-like, medicinal chemistry, telomere, telomerase, eukaryotic, nucleic acid, fluoroquinolone derivatives


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