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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 |
2011-3-3
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pubmed:abstractText |
A series of bay-substituted perylene derivatives is reported as a new class of G-quadruplex ligands. The synthesized compounds have differing N-cyclic substituents on the bay area and differing side chains on the perylene major axis. ESI-MS and FRET measurements highlighted the strongest quadruplex binders in this series and those showing the highest quadruplex/duplex selectivity. Several biological assays were performed on these compounds, which showed that compound 5 (PPL3C) triggered a DNA damage response in transformed cells with the formation of telomeric foci containing phosphorylated ?-H2AX and 53BP1. This effect mainly occurred in replicating cells and was consistent with Pot1 dissociation. Compound 5 does not induce telomere damage in normal cells, which are unaffected by treatment with the compound, suggesting that this agent preferentially kills cancer cells. These results reinforce the notion that G-quadruplex binding compounds can act as broad inhibitors of telomere-related processes and have potential as selective antineoplastic drugs.
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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 |
Mar
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:AlvinoAntonelloA,
pubmed-author:BiancoArmandodorianoA,
pubmed-author:BiroccioAnnamariaA,
pubmed-author:CasagrandeValentinaV,
pubmed-author:CiammaichellaAlinaA,
pubmed-author:D'AngeloCarmenC,
pubmed-author:FranceschinMarcoM,
pubmed-author:Ginnari-SatrianiLucaL,
pubmed-author:IachettiniSaraS,
pubmed-author:LeonettiCarloC,
pubmed-author:NeidleStephenS,
pubmed-author:OrtaggiGiancarloG,
pubmed-author:PorruManuelaM,
pubmed-author:RizzoAngelaA,
pubmed-author:SalvatiEricaE,
pubmed-author:SerrilliAnna MariaAM
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pubmed:issnType |
Electronic
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pubmed:day |
10
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1140-56
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pubmed:meshHeading |
pubmed-meshheading:21280624-Antineoplastic Agents,
pubmed-meshheading:21280624-Cell Line, Tumor,
pubmed-meshheading:21280624-Cell Proliferation,
pubmed-meshheading:21280624-Cell Survival,
pubmed-meshheading:21280624-DNA Damage,
pubmed-meshheading:21280624-Drug Screening Assays, Antitumor,
pubmed-meshheading:21280624-Fluorescence Resonance Energy Transfer,
pubmed-meshheading:21280624-G-Quadruplexes,
pubmed-meshheading:21280624-Histones,
pubmed-meshheading:21280624-Humans,
pubmed-meshheading:21280624-Ligands,
pubmed-meshheading:21280624-Perylene,
pubmed-meshheading:21280624-Phosphorylation,
pubmed-meshheading:21280624-Piperidines,
pubmed-meshheading:21280624-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:21280624-Structure-Activity Relationship,
pubmed-meshheading:21280624-Telomere
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pubmed:year |
2011
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pubmed:articleTitle |
N-cyclic bay-substituted perylene G-quadruplex ligands have selective antiproliferative effects on cancer cells and induce telomere damage.
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pubmed:affiliation |
Dipartimento di Chimica, Universita? degli Studi La Sapienza, Ple A Moro 5, 00185 Roma, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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