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

Guochun Zhou, Chiawei W. Tsai, Jun O. 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

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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