|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0007634,
umls-concept:C0013126,
umls-concept:C0020792,
umls-concept:C0023418,
umls-concept:C0090388,
umls-concept:C0162638,
umls-concept:C0332324,
umls-concept:C0872079,
umls-concept:C1328819,
umls-concept:C1421563,
umls-concept:C1704928,
umls-concept:C1999216
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|
pubmed:issue |
20
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|
pubmed:dateCreated |
2010-9-20
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|
pubmed:abstractText |
An in silico structure-based ligand design approach resulted in the identification of the first non-peptidic small molecule able to inhibit protein-protein interactions between 14-3-3 and c-Abl. This compound shows an anti-proliferative effect on human leukemia cells either sensitive or resistant to Imatinib, in consequence of the T315I mutation. It also mediates c-Abl release from 14-3-3 in a way similar to that found in response to Imatinib treatment.
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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 |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
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pubmed:issn |
1464-3405
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pubmed:author |
|
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
|
pubmed:volume |
20
|
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
6133-7
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pubmed:meshHeading |
pubmed-meshheading:20832303-14-3-3 Proteins,
pubmed-meshheading:20832303-Antineoplastic Agents,
pubmed-meshheading:20832303-Apoptosis,
pubmed-meshheading:20832303-Cell Line, Tumor,
pubmed-meshheading:20832303-Drug Resistance, Neoplasm,
pubmed-meshheading:20832303-Humans,
pubmed-meshheading:20832303-Leukemia, Myelogenous, Chronic, BCR-ABL Positive,
pubmed-meshheading:20832303-Models, Molecular,
pubmed-meshheading:20832303-Piperazines,
pubmed-meshheading:20832303-Protein Binding,
pubmed-meshheading:20832303-Protein Transport,
pubmed-meshheading:20832303-Proto-Oncogene Proteins c-abl,
pubmed-meshheading:20832303-Pyrimidines,
pubmed-meshheading:20832303-Small Molecule Libraries
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|
pubmed:year |
2010
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|
pubmed:articleTitle |
Identification of the first non-peptidic small molecule inhibitor of the c-Abl/14-3-3 protein-protein interactions able to drive sensitive and Imatinib-resistant leukemia cells to apoptosis.
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|
pubmed:affiliation |
Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Siena, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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