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| Título: | Phospho-kinase profile of colorectal tumors guides in the selection of multi-kinase inhibitors |
Autor: | Serrano-Heras, Gemma CSIC ORCID; Cuenca-López, María D.; Montero, Juan Carlos CSIC ORCID; Morales, Jorge C.; Pandiella, Atanasio CSIC ORCID CVN ; Ocaña, Alberto | Palabras clave: | EC-70124 Kinase inhibitors Colon cancer |
Fecha de publicación: | 2015 | Editor: | Impact Journals | Citación: | Oncotarget 6(31): 31272-31283 (2015) | Resumen: | Protein kinases play a central role in the oncogenesis of colorectal tumors and are attractive druggable targets. Detection of activated kinases within a tumor could open avenues for drug selection and optimization of new kinase inhibitors. By using a phosphokinase arrays with human colorectal tumors we identified activated kinases, including the Epidermal Growth Factor Receptor (EGFR), components of the PI3K/mTOR pathway (AKT and S6), and STAT, among others. A pharmacological screening with kinase inhibitors against these proteins helped us to identify a new kinase inhibitor, termed EC-70124 that showed the highest anti-proliferative activity in cell lines. EC-70124 also inhibited cell migration and biochemical experiments demonstrated its effect targeting the PI3K/mTOR pathway. This drug also arrested cells at G2/M and induced apoptosis. Experiments in combination with standard chemotherapy used in the clinical setting indicated a synergistic effect. EC-70124 also reduced tumor growth in vivo and inhibited pS6 in the implanted tumors. In conclusion, by studying the kinase profile of colorectal tumors, we identified relevant activated pathways, and a new multi-kinase compound with significant antitumor properties. | Descripción: | This is an open-access article distributed under the terms of the Creative Commons Attribution License.-- et al. | Versión del editor: | http://dx.doi.org/10.18632/oncotarget.5211 | URI: | http://hdl.handle.net/10261/135731 | DOI: | 10.18632/oncotarget.5211 | Identificadores: | doi: 10.18632/oncotarget.5211 e-issn: 1949-2553 |
| Aparece en las colecciones: | (IBMCC) Artículos |
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| Phospho-kinase.pdf | 4,57 MB | Adobe PDF |  Visualizar/Abrir |
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