Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6066
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 
Evensen, L.
Dreassi, Elena 
Zamperini, Claudio
Caporicci, M.
Falchi, Federico
Musumeci, A.
Schenone, S.
Lorens, J. B.
Botta, Maurizio 
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.
Description: 
54480
URI: http://hdl.handle.net/20.500.12779/6066
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2012.07.014
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