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Results to be published elsewhere.
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4
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33745148820
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note
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Various approaches have been tested in order to selectively inhibit the VEGF pathway. Soluble VEGF receptors (i.e. VEGF-Trap) have shown a powerful and selective antitumor action, whereas VEGF specific antibody Avastin has been successfully used as a therapeutic in several cancer indications. Other strategies focus on inhibiting the kinase activity of VEGFR2 in order to annihilate the VEGF effect.
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5
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10744221485
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more..
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7
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Petrella, E.C.9
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0035147650
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Tzung S.P., Kim K.M., Basanez G., Giedt C.D., Simon J., Zimmerberg J., Zhang K.Y., and Hockenbery D.M. Nat. Cell Biol. 3 (2001) 183
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10
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0037212039
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For additional examples of small molecules antagonizing protein-protein interactions, see;
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For additional examples of small molecules antagonizing protein-protein interactions, see;. Gadek T.R., and Nicholas J.B. Biochem. Pharmacol. 65 (2003) 1
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Biochem. Pharmacol.
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Gadek, T.R.1
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33745124206
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note
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ELISA test: Neuropilin 1 was expressed in a baculovirus system as a soluble form able to bind VEGF165, purified from High Five insect cells, and stored at -80 °C in 50% glycerol. VEGF165 was bought from R&D Systems and stored at -80 °C. The screening procedure is based on an ELISA test with Nrp1 coated on the plates and VEGF165 added for the binding assay. After several washing steps, an anti-VEGF antibody is used to detect the level of interaction between the two proteins. Detection is based on luminescence generated by an enzyme (HRP) coupled to the antibody.
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19
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33745135294
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Bedjeguelal, K.; Bienaymé, H.; Schmitt, P.; Grisoni, S. PCT Int. Appl. WO 2,004,108,722, 2004;.
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33745149558
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Bedjeguelal, K.; Bienaymé, H.; Poigny, S.; Schmitt, P.; Tam, E. QSAR Combi. Sci. 2006, in press.
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21
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0031661388
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For a similar mechanism-based three-component condensation, see:
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For a similar mechanism-based three-component condensation, see:. Bienaymé H., and Bouzid K. Angew. Chem. Int. Ed. 37 (1998) 2234
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Angew. Chem. Int. Ed.
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Bienaymé, H.1
Bouzid, K.2
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22
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20244384429
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Bon R.S., Vliet B.V., Sprenkels N.E., Schmitz R.B., de Kanter F.J., Stevens C.V., Swart M., Bickelhaupt F.M., Groen M.B., and Orru R.V.A. J. Org. Chem. 70 (2005) 3542
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Bon, R.S.1
Vliet, B.V.2
Sprenkels, N.E.3
Schmitz, R.B.4
de Kanter, F.J.5
Stevens, C.V.6
Swart, M.7
Bickelhaupt, F.M.8
Groen, M.B.9
Orru, R.V.A.10
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24
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33745145682
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note
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These activities were not the consequence of a general toxicity, as the compounds failed to show any toxicity in a LDH-release assay.
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