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ID: ALA1136797

Journal: J Med Chem

Title: Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.

Authors: Zhou G, Tsai CW, Liu JO.

Abstract: 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.

CiteXplore: 12877582

DOI: 10.1021/jm0341103