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|Title:||A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model:from in silico screening to cyclodextrin formulation||Authors:||Botta, Maurizio
Lorens, J. B.
|Keywords:||Angiogenesis Kinase Zebrafish ADME||Issue Date:||2012||Project:||None||Journal:||BIOORGANIC & MEDICINAL CHEMISTRY LETTERS||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.
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