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Design of a partial peptide mimetic of anginex with antiangiogenic and anticancer activity

By Kevin H Mayo, Ruud PM Dings, C Flader, I Nesmelova, B Hargittai, DWJ Daisy van der Schaft, LI van Eijk, D Walek, J Haseman, TR Hoye and AW Griffioen


Based on structure-activity relationships of the angiostatic ß-sheet-forming peptide anginex, we have designed a mimetic, 6DBF7, which inhibits angiogenesis and tumor growth in mice. 6DBF7 is composed of a ß-sheet-inducing dibenzofuran (DBF)-turn mimetic and two short key amino acid sequences from anginex. This novel antiangiogenic molecule is more effective in vivo than parent anginex. In a mouse xenograft model for ovarian carcinoma, 6DBF7 is observed to reduce tumor growth by up to 80%. It is suggested that the activity is based on antiangiogenesis, because in vitro tube formation is inhibited, and because treatment of tumor-bearing mice led to a significant reduction in microvessel density within the tumor. This partial peptide mimetic is the first endothelial cell-specific molecule designed as a substitute for an angiostatic inhibitory peptide

Publisher: American Society for Biochemistry and Molecular Biology Inc.
Year: 2003
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Provided by: Repository TU/e
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