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

Guochun Zhou, Chiawei W. Tsai, Jun Liu

Research output: Contribution to journalArticle

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 IC50 = 8 μM and endothelial cell proliferation with IC50 = 52 nM. With dialysis and competition assays, it was unambiguously demonstrated that binding of fumagalone to MetAP2 is reversible.

Original languageEnglish (US)
Pages (from-to)3452-3454
Number of pages3
JournalJournal of Medicinal Chemistry
Volume46
Issue number16
DOIs
StatePublished - Jul 31 2003

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Inhibitory Concentration 50
Dialysis
Endothelial cells
Cell proliferation
Biological Products
Aldehydes
Assays
Endothelial Cells
Cell Proliferation
methionine aminopeptidase 2
fumagalone
fumagillin
ovalicin

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis. / Zhou, Guochun; Tsai, Chiawei W.; Liu, Jun.

In: Journal of Medicinal Chemistry, Vol. 46, No. 16, 31.07.2003, p. 3452-3454.

Research output: Contribution to journalArticle

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