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rdf:type |
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lifeskim:mentions |
umls-concept:C0020792,
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0205314,
umls-concept:C0205360,
umls-concept:C0243077,
umls-concept:C0449445,
umls-concept:C0679622,
umls-concept:C0681836,
umls-concept:C0920425,
umls-concept:C1328819,
umls-concept:C1333893,
umls-concept:C2267219,
umls-concept:C2718090
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pubmed:issue |
21
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pubmed:dateCreated |
2009-11-5
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pubmed:abstractText |
5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h, a potent inhibitor of HDAC4 and HDAC6 (HDAC4 WT IC(50) = 310 nM, HDAC6 IC(50) = 70 nM) that displays 40-fold selectivity over HDAC1 and improved stability in HCT116 cancer cells (t(1/2) = 11 h). Compounds 6h and 2 show inhibition of alpha-tubulin deacetylation in HCT116 cells at 1 microM concentration and antiproliferation effects only at concentrations where inhibition of histone H3 deacetylation is observed.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/HDAC1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/HDAC4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/HDAC6 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylase 2,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylases,
http://linkedlifedata.com/resource/pubmed/chemical/Histones,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Repressor Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Thiophenes,
http://linkedlifedata.com/resource/pubmed/chemical/Tubulin
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:AltamuraSergioS,
pubmed-author:Di MarcoAnnaliseA,
pubmed-author:FerrignoFedericaF,
pubmed-author:JonesPhilipP,
pubmed-author:LauferRalphR,
pubmed-author:MuragliaEsterE,
pubmed-author:OntoriaJesus MJM,
pubmed-author:PalumbiMaria CeciliaMC,
pubmed-author:RowleyMichaelM,
pubmed-author:ScarpelliRitaR,
pubmed-author:Schultz-FademrechtCarstenC,
pubmed-author:SerafiniSergioS,
pubmed-author:SteinkühlerChristianC
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pubmed:issnType |
Electronic
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pubmed:day |
12
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6782-9
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pubmed:meshHeading |
pubmed-meshheading:19888759-Acetylation,
pubmed-meshheading:19888759-Antineoplastic Agents,
pubmed-meshheading:19888759-Cell Line, Tumor,
pubmed-meshheading:19888759-Cell Proliferation,
pubmed-meshheading:19888759-Dose-Response Relationship, Drug,
pubmed-meshheading:19888759-Drug Screening Assays, Antitumor,
pubmed-meshheading:19888759-Histone Deacetylase 1,
pubmed-meshheading:19888759-Histone Deacetylase 2,
pubmed-meshheading:19888759-Histone Deacetylases,
pubmed-meshheading:19888759-Histones,
pubmed-meshheading:19888759-Humans,
pubmed-meshheading:19888759-Isoenzymes,
pubmed-meshheading:19888759-Repressor Proteins,
pubmed-meshheading:19888759-Structure-Activity Relationship,
pubmed-meshheading:19888759-Thiophenes,
pubmed-meshheading:19888759-Tubulin
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pubmed:year |
2009
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pubmed:articleTitle |
Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.
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pubmed:affiliation |
Istituto Di Ricerche Di Biologia Molecolare, P. Angeletti SpA (IRBM-MRL, Rome), Via Pontina Km 30,600, I-00040 Pomezia, Italy. jmontoria@gmail.com
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Validation Studies
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