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pubmed-article:12877582pubmed:abstractTextFumagillin 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.lld:pubmed
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pubmed-article:12877582pubmed:articleTitleFumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.lld:pubmed
pubmed-article:12877582pubmed:affiliationDepartment of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA.lld:pubmed
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