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

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

Journal Name: Current Pharmaceutical Design

Volume 18 , Issue 14 , 2012

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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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Article Details

Year: 2012
Published on: 16 March, 2012
Page: [1973 - 1983]
Pages: 11
DOI: 10.2174/138161212799958369
Price: $65

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