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
Current Pharmaceutical Design
Title:Searching Drug-Like Anti-cancer Compound(s) Based on G-Quadruplex Ligands
Volume: 18 Issue: 14
Author(s): Qian Li, Jun-Feng Xiang, Hong Zhang and Ya-Lin Tang
Affiliation:
Keywords: G-quadruplex, anti-cancer, drug screening, drug-like, medicinal chemistry, telomere, telomerase, eukaryotic, nucleic acid, fluoroquinolone derivatives
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.
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Cite this article as:
Li Qian, Xiang Jun-Feng, Zhang Hong and Tang Ya-Lin, Searching Drug-Like Anti-cancer Compound(s) Based on G-Quadruplex Ligands, Current Pharmaceutical Design 2012; 18 (14) . https://dx.doi.org/10.2174/138161212799958369
DOI https://dx.doi.org/10.2174/138161212799958369 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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