1446219-98-2Relevant academic research and scientific papers
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2
Troxler, Thomas,Greenidge, Paulette,Zimmermann, Kaspar,Desrayaud, Sandrine,Drückes, Peter,Schweizer, Tatjana,Stauffer, Daniela,Rovelli, Giorgio,Shimshek, Derya R.
, p. 4085 - 4090 (2013/07/25)
Mutations in leucine-rich repeat kinase-2 (LRRK2) are the most common genetic cause of Parkinson's disease (PD). The most frequent kinase-enhancing mutation is the G2019S residing in the kinase activation domain. This opens up a promising therapeutic avenue for drug discovery targeting the kinase activity of LRRK2 in PD. Several LRRK2 inhibitors have been reported to date. Here, we report a selective, brain penetrant LRRK2 inhibitor and demonstrate by a competition pulldown assay in vivo target engagement in mice.
