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| Título: | Triazolopyrimidines Are Microtubule-Stabilizing Agents that Bind the Vinca Inhibitor Site of Tubulin |
Otros títulos: | Triazolopyrimidines stabilize microtubules by binding to the vinca inhibitor site of tubulin | Autor: | Sáez-Calvo, Gonzalo CSIC; Balaguer, Francisco de Asís CSIC ORCID; Barasoain, Isabel CSIC ; Rodríguez-Salarichs, Javier CSIC; Muñoz-Hernández, Hugo CSIC ORCID; Berbís, Manuel Álvaro CSIC; Peñalva, Miguel Ángel CSIC ORCID ; Matesanz, Ruth CSIC ; Canales, Ángeles CSIC ORCID; Jiménez-Barbero, Jesús CSIC ORCID; Andreu, José Manuel CSIC ORCID ; Díaz, José Fernando CSIC ORCID | Palabras clave: | Tubulin Microtubules Microtubule‐targeting agents Antitumourals Resistance to chemotherapy |
Fecha de publicación: | 22-jun-2017 | Editor: | Elsevier | Citación: | Cell Chemical Biology 24 (6) 737–750.e6 (2017) | Resumen: | Microtubule-targeting agents (MTAs) are some of the clinically most successful anti-cancer drugs. Unfortunately, instances of multidrug resistances to MTA have been reported, which highlights the need for developing MTAs with different mechanistic properties. One less explored class of MTAs are [1,2,4]triazolo[1,5-a]pyrimidines (TPs). These cytotoxic compounds are microtubule-stabilizing agents that inexplicably bind to vinblastine binding site on tubulin, which is typically targeted by microtubule-destabilizing agents. Here we used cellular, biochemical, and structural biology approaches to address this apparent discrepancy. Our results establish TPs as vinca-site microtubule-stabilizing agents that promote longitudinal tubulin contacts in microtubules, in contrast to classical microtubule-stabilizing agents that primarily promote lateral contacts. Additionally we observe that TPs studied here are not affected by p-glycoprotein overexpression, and suggest that TPs are promising ligands against multidrug-resistant cancer cells. | Descripción: | 53 p.-7 fig.+ 7 p.-1 tab.supl.-6 fig.supl. Saez Calvo, Gonzalo et al. | Versión del editor: | https://doi.org/10.1016/j.chembiol.2017.05.016 | URI: | http://hdl.handle.net/10261/152590 | DOI: | 10.1016/j.chembiol.2017.05.016 | ISSN: | 2451-9456 | E-ISSN: | 2451-9456 |
| Aparece en las colecciones: | (CIB) Artículos |
Ficheros en este ítem:
| Fichero | Descripción | Tamaño | Formato | |
|---|---|---|---|---|
| Saez-Calvo-et-al.2017.pdf | Artículo principal | 3,26 MB | Adobe PDF |  Visualizar/Abrir |
| Saez-Calvo-et-al.2017.mat.supl.pdf | Material suplementario | 1,05 MB | Adobe PDF |  Visualizar/Abrir |
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