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• W2407088810 abstract "// María-Dolores Canela 1 , Sam Noppen 2 , Oskía Bueno 1 , Andrea E. Prota 3 , Katja Bargsten 3 , Gonzalo Sáez-Calvo 4 , María-Luisa Jimeno 5 , Mohammed Benkheil 2 , Domenico Ribatti 6 , Sonsoles Velázquez 1 , María-José Camarasa 1 , J. Fernando Díaz 4 , Michel O. Steinmetz 3 , Eva-María Priego 1 , María-Jesús Pérez-Pérez 1 , Sandra Liekens 2 1 Instituto de Química Médica (IQM-CSIC), Madrid, Spain 2 KU Leuven – University of Leuven, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium 3 Laboratory of Biomolecular Research, Department of Biology and Chemistry, Paul Scherrer Institut, Villigen, Switzerland 4 Centro de Investigaciones Biológicas (CIB-CSIC), Madrid, Spain 5 Centro de Química Orgánica Lora-Tamayo (CENQUIOR-CSIC), Madrid, Spain 6 Department of Basic Medical Sciences, Neurosciences and Sensory Organs, University of Bari Medical School, National Cancer Institute “Giavanni Paolo II”, Bari, Italy Correspondence to: Sandra Liekens, email: sandra.liekens@kuleuven.be María-Jesús Pérez-Pérez, email: mjperez@iqm.csic.es Keywords: cancer, drug research, tubulin, vascular-disrupting Received: January 15, 2016      Accepted: May 01, 2016      Published: May 20, 2016 ABSTRACT We investigated the microtubule-destabilizing, vascular-targeting, anti-tumor and anti-metastatic activities of a new series of chalcones, whose prototype compound is (E)-3-(3’’-amino-4’’-methoxyphenyl)-1-(5’-methoxy-3’,4’-methylendioxyphenyl)-2-methylprop-2-en-1-one (TUB091). X-ray crystallography showed that these chalcones bind to the colchicine site of tubulin and therefore prevent the curved-to-straight structural transition of tubulin, which is required for microtubule formation. Accordingly, TUB091 inhibited cancer and endothelial cell growth, induced G2/M phase arrest and apoptosis at 1-10 nM. In addition, TUB091 displayed vascular disrupting effects in vitro and in the chicken chorioallantoic membrane (CAM) assay at low nanomolar concentrations. A water-soluble L-Lys-L-Pro derivative of TUB091 (i.e. TUB099) showed potent antitumor activity in melanoma and breast cancer xenograft models by causing rapid intratumoral vascular shutdown and massive tumor necrosis. TUB099 also displayed anti-metastatic activity similar to that of combretastatin A4-phosphate. Our data indicate that this novel class of chalcones represents interesting lead molecules for the design of vascular disrupting agents (VDAs). Moreover, we provide evidence that our prodrug approach may be valuable for the development of anti-cancer drugs." @default.
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• W2407088810 date "2016-05-20" @default.
• W2407088810 modified "2023-10-18" @default.
• W2407088810 title "Antivascular and antitumor properties of the tubulin-binding chalcone TUB091" @default.
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• W2407088810 doi "https://doi.org/10.18632/oncotarget.9527" @default.
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