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- W2000591073 abstract "Angiogenesis is a cellular process that involves the sprouting of new blood vessels from pre-existing ones. Fibroblast growth factors (FGFs) play a crucial role in the regulation for angiogenesis and tumor metastases. Therefore, intensive research efforts are on to develop drugs that can specifically inhibit FGF-induced angiogenesis. FGFs exhibit their cell proliferation activity by binding to the extracellular D2 domain of their cell surface receptor. Suramin has been previously shown to inhibit FGF-induced tumors. In this context, in the present study, we investigate the interaction of suramin with the extracellular D2 domain of the FGF receptor (FGFR). Results of the isothermal titration calorimetry (ITC) experiments suggest that suramin binds to the D2 domain of FGFR with a reasonably high affinity (Kd ∼ 10−6 M). ITC experiments, carried out at various salt concentrations, show that suramin-D2 domain interaction is mostly stabilized by ionic interactions. Limited trypsin digestion experiments and ANS binding experiments reveal conformational changes in the D2 domain induced by suramin binding. Equilibrium unfolding experiments monitored by fluorescence spectroscopy reveal that the D2 domain is significantly stabilized by suramin. 1H-15N chemical shift perturbation data shows that the suramin binding sites are mostly composed of residues located at the N- and C-terminal ends of the D2 domain and is supported by site-directed mutagenesis experiments. Interestingly, some of the residues that bind to suramin are located at the FGF-D2 domain interface. A structural model of the suramin D2 domain complex is generated from the experimental data. It appears that suramin inhibits cell proliferation activity of FGF by preventing its interaction with FGFR. The results of this study are expected to pave the way for a rational design of drugs against FGF-induced tumors." @default.
- W2000591073 created "2016-06-24" @default.
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- W2000591073 date "2009-02-01" @default.
- W2000591073 modified "2023-09-27" @default.
- W2000591073 title "Understanding the Mechanism of the Anti-angiogenic Activity of Suramin" @default.
- W2000591073 doi "https://doi.org/10.1016/j.bpj.2008.12.3143" @default.
- W2000591073 hasPublicationYear "2009" @default.
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