PUBLICATION
Biological and Pharmacological Characterization of Benzothiazole-Based CK-1δ Inhibitors in Models of Parkinson's Disease
- Authors
- Morales-Garcia, J.A., Salado, I.G., Sanz-San Cristobal, M., Gil, C., Pérez-Castillo, A., Martínez, A., Pérez, D.I.
- ID
- ZDB-PUB-180720-8
- Date
- 2017
- Source
- ACS omega 2: 5215-5220 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
- none
- PubMed
- 30023743 Full text @ ACS Omega
Citation
Morales-Garcia, J.A., Salado, I.G., Sanz-San Cristobal, M., Gil, C., Pérez-Castillo, A., Martínez, A., Pérez, D.I. (2017) Biological and Pharmacological Characterization of Benzothiazole-Based CK-1δ Inhibitors in Models of Parkinson's Disease. ACS omega. 2:5215-5220.
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.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping