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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
26
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pubmed:dateCreated |
2006-12-21
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pubmed:abstractText |
A potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase mimetic (SM-131, 2) has been designed, synthesized, and evaluated. Compound 2 binds to X-linked inhibitors of apoptosis proteins (XIAP) with a Ki of 61 nM in a competitive binding assay and directly antagonizes the XIAP inhibition of caspase-9 activity in a cell-free functional assay. Compound 2 achieves an IC50 of 100 nM in inhibition of cell growth and effectively induces cell death in the MDA-MB-231 human breast cancer cell line.
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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 |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7916-20
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pubmed:dateRevised |
2007-12-3
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pubmed:meshHeading |
pubmed-meshheading:17181177-Azepines,
pubmed-meshheading:17181177-Binding, Competitive,
pubmed-meshheading:17181177-Breast Neoplasms,
pubmed-meshheading:17181177-Caspase 3,
pubmed-meshheading:17181177-Caspase 9,
pubmed-meshheading:17181177-Cell Death,
pubmed-meshheading:17181177-Cell Membrane Permeability,
pubmed-meshheading:17181177-Cell Proliferation,
pubmed-meshheading:17181177-Enzyme Activation,
pubmed-meshheading:17181177-Heterocyclic Compounds,
pubmed-meshheading:17181177-Humans,
pubmed-meshheading:17181177-Inhibitor of Apoptosis Proteins,
pubmed-meshheading:17181177-Mitochondria,
pubmed-meshheading:17181177-Models, Molecular,
pubmed-meshheading:17181177-Molecular Conformation,
pubmed-meshheading:17181177-Molecular Mimicry,
pubmed-meshheading:17181177-Protein Binding,
pubmed-meshheading:17181177-Pyrrolidines,
pubmed-meshheading:17181177-Structure-Activity Relationship,
pubmed-meshheading:17181177-Tumor Cells, Cultured,
pubmed-meshheading:17181177-X-Linked Inhibitor of Apoptosis Protein
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pubmed:year |
2006
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pubmed:articleTitle |
Design, synthesis, and evaluation of a potent, cell-permeable, conformationally constrained second mitochondria derived activator of caspase (Smac) mimetic.
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pubmed:affiliation |
Comprehensive Cancer Center, Department of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI 48109, 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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