Source:http://linkedlifedata.com/resource/pubmed/id/18497981
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2008-5-23
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| pubmed:abstractText |
Human chronic myelogenous leukemia (CML) is a malignancy of pluripotent hematopoietic cells characterized by a distinctive cytogenetic abnormality resulting in the creation of a p210 Bcr-Abl fusion protein with abnormal tyrosine kinase activity. Recently, a selective Abl kinase inhibitor, Imatinib mesylate, was introduced as a first line therapy for CML. Despite the initial response, CML patients develop a resistantance to Imatinib, which is mediated mainly by point mutations within the Abl protein. Herein, we describe the identification of mycelium organic extracts of Daedalea gibbosa with selective anti-proliferating and apoptosis-inducing activities against K562 cells and other laboratory model of CML. Using activity-guided purification, we isolated an active fraction, F6, which inhibits in vitro kinase activity of recombinant Abl. The active fraction significantly inhibits the autophosphorylation of native and mutated Bcr-Abl, which are resistant to Imatinib treatment including the T315I mutation. Using a colony-forming assay, we demonstrated that the active fraction is effective in inhibiting the colony formation of the Ba/F3 cell line harboring either native Bcr-Abl or its mutations, including the T315I mutation. Our data illustrated the potential of natural products in cancer therapeutics.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Bcr-Abl tyrosine kinase,
http://linkedlifedata.com/resource/pubmed/chemical/Fungal Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Fusion Proteins, bcr-abl,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Tyrosine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Proto-Oncogene Proteins c-abl,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/imatinib
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| pubmed:status |
MEDLINE
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| pubmed:month |
Jun
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| pubmed:issn |
1019-6439
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
32
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
1197-204
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| pubmed:dateRevised |
2009-11-19
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| pubmed:meshHeading |
pubmed-meshheading:18497981-Agaricales,
pubmed-meshheading:18497981-Animals,
pubmed-meshheading:18497981-Apoptosis,
pubmed-meshheading:18497981-Blotting, Western,
pubmed-meshheading:18497981-Cell Differentiation,
pubmed-meshheading:18497981-Cell Proliferation,
pubmed-meshheading:18497981-Cells, Cultured,
pubmed-meshheading:18497981-Colony-Forming Units Assay,
pubmed-meshheading:18497981-Enzyme-Linked Immunosorbent Assay,
pubmed-meshheading:18497981-Fungal Proteins,
pubmed-meshheading:18497981-Fusion Proteins, bcr-abl,
pubmed-meshheading:18497981-Humans,
pubmed-meshheading:18497981-K562 Cells,
pubmed-meshheading:18497981-Mice,
pubmed-meshheading:18497981-Mutation,
pubmed-meshheading:18497981-Phosphorylation,
pubmed-meshheading:18497981-Piperazines,
pubmed-meshheading:18497981-Protein-Tyrosine Kinases,
pubmed-meshheading:18497981-Proto-Oncogene Proteins c-abl,
pubmed-meshheading:18497981-Pyrimidines
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| pubmed:year |
2008
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| pubmed:articleTitle |
Substances from the medicinal mushroom Daedalea gibbosa inhibit kinase activity of native and T315I mutated Bcr-Abl.
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| pubmed:affiliation |
Cancer Drug Discovery Program, Migal, Galilee Technology Center, Kiryat Shmona 11016, Israel.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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