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Título: | Biological and pharmacological characterization of benzothiazole-based CK-1δ inhibitors in models of Parkinson’s disease |
Autor: | Morales-García, José A. CSIC ORCID; Salado, Irene G. CSIC; Sanz-SanCristóbal, Marina CSIC; Gil, Carmen CSIC ORCID ; Pérez Castillo, Ana CSIC ORCID; Martínez Gil, Ana CSIC ORCID ; Pérez, Daniel I. CSIC ORCID | Palabras clave: | Drug discovery and Drug delivery systems Heterocyclic compounds Structure-activity relationship |
Fecha de publicación: | 30-ago-2017 | Editor: | American Chemical Society | Citación: | ACS Omega 2(8): 5215–5220 (2017) | Resumen: | Parkinson’s disease (PD), an age-related neurodegenerative disorder that results from a progressive loss of dopaminergic neurons has an enormous economical and human cost. Unfortunately, only symptomatic treatment such as dopamine replacement therapy is available. Therefore, drugs with new mechanisms of action able to protect against neuronal cell death are an urgent need. We here report the in vivo efficacy on dopaminergic neuronal protection in a PD mouse model and the lack of toxicity in zebrafish and Ames test of benzothiazole-based casein kinase-1δ (CK-1δ) nanomolar inhibitors. On the basis of these results, we propose protein kinase CK-1δ inhibitors as the possible disease-modifying drugs for PD, benzothiazole 4 being a promising drug candidate for further development as a new therapy of this neurodegenerative disease. | Versión del editor: | http://dx.doi.org/10.1021/acsomega.7b00869 | URI: | http://hdl.handle.net/10261/154777 | DOI: | 10.1021/acsomega.7b00869 | E-ISSN: | 2470-1343 |
Aparece en las colecciones: | (CIB) Artículos (IIBM) Artículos |
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