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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2009-2-6
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pubmed:databankReference |
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pubmed:abstractText |
A series of platinum(II) complexes containing dipyridophenazine (dppz) and C-deprotonated 2-phenylpyridine (N-CH) ligands were prepared and assayed for G-quadruplex DNA binding activities. [PtII(dppz-COOH)(N-C)]CF3SO3 (1; dppz-COOH = 11-carboxydipyrido[3,2-a:2',3'-c]phenazine) binds G-quadruplex DNA through an external end-stacking mode with a binding affinity of approximately 10(7) dm3 mol-1. G-quadruplex DNA binding is accompanied by up to a 293-fold increase in the intensity of photoluminescence at lambdamax = 512 nm. Using a biotinylated-primer extension telomerase assay, 1 was shown to be an effective inhibitor of human telomerase in vitro, with a telIC50 value of 760 nM.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1520-5126
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
11
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pubmed:volume |
131
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1835-46
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18998644-Cell Line,
pubmed-meshheading:18998644-DNA,
pubmed-meshheading:18998644-Electrophoresis, Polyacrylamide Gel,
pubmed-meshheading:18998644-Enzyme Inhibitors,
pubmed-meshheading:18998644-G-Quadruplexes,
pubmed-meshheading:18998644-HeLa Cells,
pubmed-meshheading:18998644-Humans,
pubmed-meshheading:18998644-Ligands,
pubmed-meshheading:18998644-Models, Molecular,
pubmed-meshheading:18998644-Nuclear Magnetic Resonance, Biomolecular,
pubmed-meshheading:18998644-Organoplatinum Compounds,
pubmed-meshheading:18998644-Phenazines,
pubmed-meshheading:18998644-Pyridines,
pubmed-meshheading:18998644-Spectrophotometry, Ultraviolet,
pubmed-meshheading:18998644-Titrimetry,
pubmed-meshheading:18998644-Topoisomerase I Inhibitors
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pubmed:year |
2009
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pubmed:articleTitle |
Platinum(II) complexes with dipyridophenazine ligands as human telomerase inhibitors and luminescent probes for G-quadruplex DNA.
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pubmed:affiliation |
Department of Chemistry and Open Laboratory of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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