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Título

Benzothiazole-based LRRK2 inhibitors as Wnt enhancers and promoters of oligodendrocytic fate

AutorZaldívar-Díez, Josefa CSIC ORCID; Li, Lingling CSIC; García, Ana M. CSIC ORCID; Zhao, Wenning; Medina-Menendez, Cristina; Haggarty, Stephen J.; Gil, Carmen CSIC ORCID ; Morales, Aixa V. CSIC ORCID; Martínez Gil, Ana CSIC ORCID
Palabras claveLRRK2 inhibitors
Adult neurogenesis
Wnt enhancers
Oligodendrocyte differentiation
Fecha de publicación11-dic-2019
EditorAmerican Chemical Society
CitaciónJournal of Medicinal Chemistry 63 (5) 2638-2655 (2020)
ResumenLeucine Rich Repeat Kinase 2 (LRRK2) is an enigmatic enzyme and a relevant target for Parkinson’s Disease (PD). However, despite the significant amount of research done in the last decade, the precise function of LRRK2 remains largely unknown. Moreover, the therapeutic potential of its inhibitors is in its infancy with the first clinical trial having just started. In the present work the molecular mechanism of LRRK2 in the control of neurogenesis or gliogenesis was investigated. We designed and synthesized novel benzothiazole-based LRRK2 inhibitors and showed that they can modulate the Wnt/β-catenin signaling pathway. Furthermore, compounds 5 and 14 were able to promote neural progenitors proliferation and drive their differentiation towards neuronal and oligodendrocytic cell fates. These results suggest potential new avenues for the application of LRRK2 inhibitors in demyelinating diseases in which oligodendrocyte cell-death is one of the pathological features.
Descripción63 p.-15 fig.-1 tab.-2 schem.
Versión del editorhttps://doi.org/10.1021/acs.jmedchem.9b01752
URIhttp://hdl.handle.net/10261/197077
DOI10.1021/acs.jmedchem.9b01752
ISSN0022-2623
E-ISSN1520-4804
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