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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2008-6-13
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pubmed:abstractText |
Hybrids of 1-deoxynojirimycin (DNJ) and aryl-1,2,3-triazole have been synthesized with a view to identifying an inhibitor of both alpha-glucosidase and methionine aminopeptidase 2 (MetAP2). One compound was a potent inhibitor of alpha-glucosidase at both the enzyme and cellular level, and this agent also inhibited bovine aortic endothelial cell (BAEC) growth and tube formation. The anti-proliferative activity of this hybrid is due to its ability to induce cell-cycle arrest in the G(1) phase. The novel agent caused a reduction in the expression of cyclin D1 but did not promote apoptosis or inhibit the phosphorylation of ERK1/2. These observations indicate that its mechanism of action is distinct from fumagillin and its analogues, which inhibit MetAP2. Stress-fibre assembly in BAECs was abolished by the novel agent indicating that the inhibition of BAEC tube formation observed is partially a result of a reduction in cell motility.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/1-Deoxynojirimycin,
http://linkedlifedata.com/resource/pubmed/chemical/Aminopeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Angiogenesis Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclin D1,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Metalloendopeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Mitogen-Activated Protein Kinase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Mitogen-Activated Protein Kinase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Triazoles,
http://linkedlifedata.com/resource/pubmed/chemical/alpha-Glucosidases,
http://linkedlifedata.com/resource/pubmed/chemical/methionine aminopeptidase 2
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3391
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6333-7
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18504133-1-Deoxynojirimycin,
pubmed-meshheading:18504133-Aminopeptidases,
pubmed-meshheading:18504133-Angiogenesis Inhibitors,
pubmed-meshheading:18504133-Animals,
pubmed-meshheading:18504133-Aorta,
pubmed-meshheading:18504133-Apoptosis,
pubmed-meshheading:18504133-Cattle,
pubmed-meshheading:18504133-Cell Cycle,
pubmed-meshheading:18504133-Cell Line,
pubmed-meshheading:18504133-Cell Movement,
pubmed-meshheading:18504133-Cell Proliferation,
pubmed-meshheading:18504133-Cyclin D1,
pubmed-meshheading:18504133-Endothelial Cells,
pubmed-meshheading:18504133-Enzyme Inhibitors,
pubmed-meshheading:18504133-Metalloendopeptidases,
pubmed-meshheading:18504133-Mitogen-Activated Protein Kinase 1,
pubmed-meshheading:18504133-Mitogen-Activated Protein Kinase 3,
pubmed-meshheading:18504133-Neovascularization, Pathologic,
pubmed-meshheading:18504133-Neovascularization, Physiologic,
pubmed-meshheading:18504133-Phosphorylation,
pubmed-meshheading:18504133-Stress Fibers,
pubmed-meshheading:18504133-Triazoles,
pubmed-meshheading:18504133-alpha-Glucosidases
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pubmed:year |
2008
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pubmed:articleTitle |
Hybrids of 1-deoxynojirimycin and aryl-1,2,3-triazoles and biological studies related to angiogenesis.
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pubmed:affiliation |
UCD School of Biomolecular and Biomedical Science and the UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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