Journal
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 78, Issue -, Pages 149-156Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijbiomac.2015.03.034
Keywords
G-quadruplex; Phenanthroline derivative; Selectivity
Funding
- Major National Basic Research Projects [2013CB7337010]
- Major Research Program of National Natural Science Foundation of China [91027033s]
- Key Program of the Chinese Academy of Sciences [KJCX2-EW-N06-01]
- National Natural Science Foundation of China [21302188]
- Strategic Priority Research Program of the Chinese Academy of Sciences [XDA09030307]
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A key problem in designing G-quadruplex ligand is how to discriminate quadruplex DNA specifically from other DNAs, searching ligands targeted at special G-quadruplex structure with high selectivity is a major challenge. Herein, a phenanthrolin-dicarboxylate ester (PD) is proved to exhibit selectivity toward parallel and hybrid G-quadruplex structures with propeller and edge-wise loops, over duplex DNA and antiparallel quadruplex structure with diagonal loop. Such preferred binding of PD to these special G-quadruplex structures is possibly resulted from steric hindrance of: (1) the four substituent groups in PD molecule which prevent close interaction with duplex DNA and (2) the diagonal loop above the G-tetrads in antiparallel G-quadruplex which hinder face-to-face stacking of planar phenanthrolin ring to G-tetrads. In line with its stabilizing ability of G-quadruplex, PD molecule exhibit a inhibitory ability telomerase activity, as well as the potent cytotoxic activity against several human cancer cell lines, which makes it an interesting anti-tumor drug lead. (C) 2015 Elsevier B.V. All rights reserved.
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