Xianming Deng, Nicolas Dzamko, A. Prescott
Mar 6, 2011
Citations
35
Influential Citations
391
Citations
Quality indicators
Journal
Nature chemical biology
Abstract
Mutations in leucine-rich repeat kinase 2 (LRRK2) are strongly associated with late-onset autosomal dominant Parkinson’s disease. We employed a novel, parallel, compound-centric approach to identify a potent and selective LRRK2 inhibitor LRRK2-IN-1, and demonstrated that inhibition of LRRK2 induces dephosphorylation of Ser910/Ser935 and accumulation of LRRK2 within aggregate structures. LRRK2-IN-1 will serve as a versatile tool to pharmacologically interrogate LRRK2 biology and study its role in Parkinson’s disease.