FIGURE 7.

Endorepellin attenuates VEGFR2 and VEGFA transcription in PAE-VEGFR2 cells. A, representative co-immunoprecipitation (IP) studies of VEGFR2 from PAE-VEGFR2 immunoblotted (IB) with antibodies against VEGFR2 p-Tyr-1175, total VEGFR2, or SHP-1. Note that endorepellin attenuates the ligand-mediated activation of VEGFR2 but also enhances the recruitment of SHP-1 to VEGFR2. B and C, quantification of co-immunoprecipitation studies similar to those shown in A. The values represent the mean ± S.E. of four independent experiments. *, p < 0.05; **, p < 0.01. D, transcriptional inhibition of VEGFA by endorepellin. Mass cultures of stably transfected PAE-VEGFR2^VEGF-Luc cells were exposed for 4 h to VEGFA, endorepellin, or in combination. Note that endorepellin suppresses VEGFA-driven luciferase activity and counteracts the stimulatory effects of VEGFA. The values were normalized on PBS-treated controls and represent the means + S.E. from four experiments run in triplicate. *, p < 0.05; **, p < 0.01. E, qPCR trials evaluating firefly luciferase expression in PAE-VEGFR2^VEGF-Luc after treatment with 100 nm endorepellin for 4 h. The values were normalized on ACTB (β-actin) mRNA levels and are representative of two trials run in quadruplicate. ***, p < 0.001.