2. Academic Validation
  3. Biological and Pharmacological Characterization of Benzothiazole-Based CK-1δ Inhibitors in Models of Parkinson's Disease

Biological and Pharmacological Characterization of Benzothiazole-Based CK-1δ Inhibitors in Models of Parkinson's Disease

  • ACS Omega. 2017 Aug 31;2(8):5215-5220. doi: 10.1021/acsomega.7b00869.
José A Morales-Garcia 1 2 3,  Irene G Salado 4,  Marina Sanz-San Cristobal 1 2,  Carmen Gil 4,  Ana Pérez-Castillo 1 2,  Ana Martínez 4,  Daniel I Pérez 4
Affiliations

Affiliations

  • 1 Instituto de Investigaciones Biomédicas CSIC-UAM, Arturo Duperier, 4, 28029 Madrid, Spain.
  • 2 Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas (CIBERNED), 28031 Madrid, Spain.
  • 3 Departamento de Biología Celular, Facultad de Medicina, UCM, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
  • 4 IPSBB Unit, Centro de Investigaciones Biológicas-CSIC, Ramiro de Maeztu 9, 28040 Madrid, Spain.
PMID: 30023743 DOI: 10.1021/acsomega.7b00869
Abstract

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.

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