Small-Molecule Inhibitors of LRRK2.
Adv Neurobiol
; 14: 241-264, 2017.
Article
en En
| MEDLINE
| ID: mdl-28353288
ABSTRACT
Mutations in the leucine-rich repeat kinase 2 (LRRK2) protein have been genetically and functionally linked to Parkinson's disease (PD). The kinase activity of LRRK2 is increased by pathogenic mutations; therefore, modulation of LRRK2 kinase activity by a selective small-molecule inhibitor has been proposed as a potentially viable treatment for Parkinson's disease. This chapter presents a historical overview of the development and bioactivity of several small-molecule LRRK2 inhibitors that have been used to inhibit LRRK2 kinase activity in vitro or in vivo. These compounds are important tools for understanding the cellular biology of LRRK2 and for evaluating the potential of LRRK2 inhibitors as disease-modifying PD therapies.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Proteínas Quinasas
/
Proteína 2 Quinasa Serina-Treonina Rica en Repeticiones de Leucina
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Adv Neurobiol
Año:
2017
Tipo del documento:
Article
País de afiliación:
Estados Unidos