rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
16
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pubmed:dateCreated |
2003-7-24
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pubmed:abstractText |
Fumagillin and ovalicin constitute a family of structurally related natural products that possess antiangiogenic activity. We report the synthesis of a new fumagillin analogue, fumagalone, in which the spiroepoxide group is replaced with an aldehyde. Fumagalone inhibits type 2 methionine aminopeptidase (MetAP2) with IC(50) = 8 microM and endothelial cell proliferation with IC(50) = 52 nM. With dialysis and competition assays, it was unambiguously demonstrated that binding of fumagalone to MetAP2 is reversible.
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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/Aminopeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Angiogenesis Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclohexanes,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclohexanones,
http://linkedlifedata.com/resource/pubmed/chemical/Epoxy Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Fatty Acids, Unsaturated,
http://linkedlifedata.com/resource/pubmed/chemical/Metalloendopeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Sesquiterpenes,
http://linkedlifedata.com/resource/pubmed/chemical/fumagillin,
http://linkedlifedata.com/resource/pubmed/chemical/methionine aminopeptidase 2
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
31
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3452-4
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12877582-Aminopeptidases,
pubmed-meshheading:12877582-Angiogenesis Inhibitors,
pubmed-meshheading:12877582-Animals,
pubmed-meshheading:12877582-Cattle,
pubmed-meshheading:12877582-Cell Division,
pubmed-meshheading:12877582-Cyclohexanes,
pubmed-meshheading:12877582-Cyclohexanones,
pubmed-meshheading:12877582-Endothelium, Vascular,
pubmed-meshheading:12877582-Epoxy Compounds,
pubmed-meshheading:12877582-Fatty Acids, Unsaturated,
pubmed-meshheading:12877582-Metalloendopeptidases,
pubmed-meshheading:12877582-Protein Binding,
pubmed-meshheading:12877582-Sesquiterpenes
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pubmed:year |
2003
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pubmed:articleTitle |
Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.
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pubmed:affiliation |
Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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