2024-03-29T00:48:38Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/1547772020-08-12T13:37:25Zcom_10261_86com_10261_1com_10261_22col_10261_339col_10261_275
DIGITAL.CSIC
author
Morales-García, José A.
author
Salado, Irene G.
author
Sanz-SanCristóbal, Marina
author
Gil, Carmen
author
Pérez Castillo, Ana
author
Martínez, Ana
author
Pérez, Daniel I.
funder
Ministerio de Economía y Competitividad (España)
funder
Ministerio de Economía, Industria y Competitividad (España)
funder
Consejo Superior de Investigaciones Científicas (España)
funder
Instituto de Salud Carlos III
2017-09-05T12:18:57Z
2017-09-05T12:18:57Z
2017-08-30
ACS Omega 2(8): 5215–5220 (2017)
http://hdl.handle.net/10261/154777
10.1021/acsomega.7b00869
2470-1343
http://dx.doi.org/10.13039/501100004587http://dx.doi.org/10.13039/501100003329http://dx.doi.org/10.13039/501100003339http://dx.doi.org/10.13039/501100010198
30023743
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.
eng
openAccess
Drug discovery and Drug delivery systems
Heterocyclic compounds
Structure-activity relationship
Biological and pharmacological characterization of benzothiazole-based CK-1δ inhibitors in models of Parkinson’s disease
artículo
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URL
https://digital.csic.es/bitstream/10261/154777/1/acsomega.7b00869.pdf
File
MD5
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application/pdf
acsomega.7b00869.pdf