2. Academic Validation
  3. Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo

Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo

  • J Med Chem. 2006 Sep 21;49(19):5645-8. doi: 10.1021/jm060559v.
Jun Lu 1,  Curtis R Chong,  Xiaoyi Hu,  Jun O Liu
Affiliations

Affiliation

  • 1 Department of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.
PMID: 16970390 DOI: 10.1021/jm060559v
Abstract

The fumagillin family of natural products inhibits angiogenesis through the irreversible inhibition of the type 2 methionine Aminopeptidase (MetAP2). Herein is reported a novel fumagillin analogue named fumarranol. It is shown that, like fumagillin, fumarranol selectively inhibits MetAP2 and endothelial cell proliferation. It is also active in a mouse model of angiogenesis in vivo. Unlike TNP-470, fumarranol does not covalently bind to MetAP2. Fumarranol may serve as a lead for a new class of angiogenesis inhibitors.

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