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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2011-1-28
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pubmed:abstractText |
Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematologic malignancies, including multiple myeloma (MM). Here, we report the identification of STF-083010, a novel small-molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. Treatment with STF-083010 showed significant antimyeloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells compared with other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anticancer therapy, especially in the context of MM.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
AIM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Boronic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Cytotoxins,
http://linkedlifedata.com/resource/pubmed/chemical/ERN1 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Endoribonucleases,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Serine-Threonine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazines,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides,
http://linkedlifedata.com/resource/pubmed/chemical/Thiophenes,
http://linkedlifedata.com/resource/pubmed/chemical/bortezomib
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1528-0020
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pubmed:author |
pubmed-author:BouleyDonna MDM,
pubmed-author:DenkoNicholas CNC,
pubmed-author:KoongAlbert CAC,
pubmed-author:LustSofieS,
pubmed-author:NiwaMahoM,
pubmed-author:OffnerFritzF,
pubmed-author:OlsonMichaelM,
pubmed-author:PapandreouIoannaI,
pubmed-author:Solow-CorderoDavid EDE,
pubmed-author:TamArvinA,
pubmed-author:Van MelckebekeHeleenH
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pubmed:issnType |
Electronic
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pubmed:day |
27
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pubmed:volume |
117
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1311-4
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pubmed:dateRevised |
2011-3-24
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pubmed:meshHeading |
pubmed-meshheading:21081713-Animals,
pubmed-meshheading:21081713-Antineoplastic Combined Chemotherapy Protocols,
pubmed-meshheading:21081713-Boronic Acids,
pubmed-meshheading:21081713-Cells, Cultured,
pubmed-meshheading:21081713-Cytotoxins,
pubmed-meshheading:21081713-Dose-Response Relationship, Drug,
pubmed-meshheading:21081713-Endoribonucleases,
pubmed-meshheading:21081713-Humans,
pubmed-meshheading:21081713-Mice,
pubmed-meshheading:21081713-Models, Biological,
pubmed-meshheading:21081713-Multiple Myeloma,
pubmed-meshheading:21081713-Protein Kinase Inhibitors,
pubmed-meshheading:21081713-Protein-Serine-Threonine Kinases,
pubmed-meshheading:21081713-Pyrazines,
pubmed-meshheading:21081713-Substrate Specificity,
pubmed-meshheading:21081713-Sulfonamides,
pubmed-meshheading:21081713-Thiophenes,
pubmed-meshheading:21081713-Xenograft Model Antitumor Assays
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pubmed:year |
2011
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pubmed:articleTitle |
Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma.
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pubmed:affiliation |
Department of Radiation Oncology, Stanford University School of Medicine, 269 Campus Drive, Stanford, CA 94305, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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