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VEGFR2 mutants to inhibit angiogenesis

In order to achieve a specific blockade of VEGF-induced tumour angiogenesis and also to maintain vascular permeability, which would be important for combination therapies with cytostatic compounds, partner 3 and 7 mutated VEGFR1 and targeted the tyrosine residues in the intracellular domain of the VEGFR-2. For a detailed and systematic functional analysis of single tyrosine groups in signalling all tyrosine groups were exchanged against phenylalanine in the murine VEGFR-2 and these VEGFR-2 mutants transfected into human endothelial cells (EC) for Western blot analysis.

Heidenreich R, Machein M, Nicolaus A, Hilbig A, Wild C, Clauss M, Plate KH, Breier G. Inhibition of solid tumor growth by gene transfer of VEGF receptor-1 mutants. Int J Cancer 2004;111:348-57. VEGFR2 data so far unpublished.

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