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rdf:type |
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lifeskim:mentions |
umls-concept:C0014898,
umls-concept:C0053355,
umls-concept:C0185125,
umls-concept:C0220781,
umls-concept:C0243071,
umls-concept:C0303920,
umls-concept:C0439851,
umls-concept:C1167622,
umls-concept:C1332414,
umls-concept:C1514562,
umls-concept:C1552596,
umls-concept:C1880389,
umls-concept:C1883204,
umls-concept:C1883221,
umls-concept:C1883254,
umls-concept:C1947931
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pubmed:issue |
11
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pubmed:dateCreated |
2008-5-30
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pubmed:abstractText |
Overexpression of cIAP1 correlates with resistance to radiotherapy and chemotherapy in various cancers. Recently, we reported that a class of bestatin ester analogs represented by MeBS (2) destabilized and promoted the degradation of cIAP1 through auto-ubiquitination, and thereby sensitized cancer cells to apoptosis. Herein, we present chemical evidence that bestatin ester analogs directly interact with the cIAP1-BIR3 domain by means of fluorescence polarization assay and photoaffinity labeling assay using fluorescent probes.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3354-8
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pubmed:meshHeading |
pubmed-meshheading:18448338-Aminopeptidases,
pubmed-meshheading:18448338-Apoptosis,
pubmed-meshheading:18448338-Fluorescence Polarization,
pubmed-meshheading:18448338-Inhibitor of Apoptosis Proteins,
pubmed-meshheading:18448338-Leucine,
pubmed-meshheading:18448338-Leucyl Aminopeptidase,
pubmed-meshheading:18448338-Molecular Structure,
pubmed-meshheading:18448338-Photoaffinity Labels,
pubmed-meshheading:18448338-Tumor Cells, Cultured,
pubmed-meshheading:18448338-Ubiquitination
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pubmed:year |
2008
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pubmed:articleTitle |
Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs.
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pubmed:affiliation |
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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