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EnglishA combined targeted/phenotypic approach for the rapid identification of novel antiangiogenics with in vivo efficacy is herein reported. Considering the important role played by the tyrosine kinase c-Src in the regulation of tumour angiogenesis, we submitted our in-house library of c-Src inhibitors to a sequential screening approach: in silico screening on VEGFR2, in vitro screening on HUVEC cells, ADME profiling, formulation and in vivo testing on a zebrafish model. A promising antiangiogenic candidate able to interfere with the vascular growth of a zebrafish model at low micromolar concentration was thus identified.
A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: From in silico screening to cyclodextrin formulation. / Radi M; Evensen L; Dreassi E; Zamperini C; Caporicci M; Falchi F; Musumeci F; Schenone S; Lorens JB; Botta M.. - STAMPA. - 22(2012), pp. 5579-5583.
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| Titolo: | A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: From in silico screening to cyclodextrin formulation. | |
| Autori: | ||
| Data di pubblicazione: | 2012 | |
| Rivista: | ||
| Citazione: | A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: From in silico screening to cyclodextrin formulation. / Radi M; Evensen L; Dreassi E; Zamperini C; Caporicci M; Falchi F; Musumeci F; Schenone S; Lorens JB; Botta M.. - STAMPA. - 22(2012), pp. 5579-5583. | |
| Abstract: | A combined targeted/phenotypic approach for the rapid identification of novel antiangiogenics with in vivo efficacy is herein reported. Considering the important role played by the tyrosine kinase c-Src in the regulation of tumour angiogenesis, we submitted our in-house library of c-Src inhibitors to a sequential screening approach: in silico screening on VEGFR2, in vitro screening on HUVEC cells, ADME profiling, formulation and in vivo testing on a zebrafish model. A promising antiangiogenic candidate able to interfere with the vascular growth of a zebrafish model at low micromolar concentration was thus identified. | |
| Handle: | http://hdl.handle.net/11567/468318 | |
| Appare nelle tipologie: | 01.01 - Articolo su rivista |
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