Source:http://linkedlifedata.com/resource/pubmed/id/19686236
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
2009-10-16
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pubmed:abstractText |
The 90 kD heat shock protein (Hsp90) molecular chaperone sustains multiple components of oncogenic pathways and has recently emerged as a therapeutic target that is now being clinically tested in a number of malignancies. In order to address formulation issues and to deal with possible resistance mechanisms against small molecule Hsp90 inhibitors, a range of compounds based on different molecular scaffolds are now being developed. The present study preclinically tested the effects of the novel 2-aminothienopyrimidine class Hsp90 inhibitor NVP-BEP800, which is suitable for oral formulations, on multiple myeloma cells from established cell lines and on a larger cohort (n = 40) of primary myeloma samples. The drug effectively and specifically killed the majority of primary myeloma cells in coculture with bone marrow stromal cells and reliably entailed molecular consequences of Hsp90 blockade - such as survival pathway breakdown and client protein depletion - in multiple myeloma cells from cell lines as well as from patients. Collectively, the properties of this novel drug support clinical testing in multiple myeloma.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1365-2141
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pubmed:author |
pubmed-author:BargouRalf CRC,
pubmed-author:ChatterjeeManikM,
pubmed-author:EinseleHermannH,
pubmed-author:Garcia-EcheverriaCarlosC,
pubmed-author:GrellaEvelynE,
pubmed-author:JensenMichael RMR,
pubmed-author:LangerChristianC,
pubmed-author:MüllerSabineS,
pubmed-author:QuadtCorneliaC,
pubmed-author:SchoepferJosephJ,
pubmed-author:SeggewissRuthR,
pubmed-author:StühmerThorstenT
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pubmed:issnType |
Electronic
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pubmed:volume |
147
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
319-27
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pubmed:meshHeading |
pubmed-meshheading:19686236-Antineoplastic Combined Chemotherapy Protocols,
pubmed-meshheading:19686236-Bone Marrow Cells,
pubmed-meshheading:19686236-Cell Death,
pubmed-meshheading:19686236-Coculture Techniques,
pubmed-meshheading:19686236-Dose-Response Relationship, Drug,
pubmed-meshheading:19686236-Drug Evaluation, Preclinical,
pubmed-meshheading:19686236-HSP90 Heat-Shock Proteins,
pubmed-meshheading:19686236-Humans,
pubmed-meshheading:19686236-Multiple Myeloma,
pubmed-meshheading:19686236-Neoplasm Proteins,
pubmed-meshheading:19686236-Pyrimidines,
pubmed-meshheading:19686236-Stromal Cells,
pubmed-meshheading:19686236-Tumor Cells, Cultured
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pubmed:year |
2009
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pubmed:articleTitle |
Anti-myeloma activity of the novel 2-aminothienopyrimidine Hsp90 inhibitor NVP-BEP800.
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pubmed:affiliation |
Department of Internal Medicine II, Division of Haematology, University Hospital Würzburg, Würzburg, Bavaria, Germany. stuehmer_t@medizin.uni-wuerzburg.de
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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