Article
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
Nature chemical biology - 1 Apr 2011
Deng Xianming, Dzamko Nicolas, Prescott Alan, Davies Paul, Liu Qingsong, Yang Qingkai, Lee Jiing-Dwan, Patricelli Matthew P, Nomanbhoy Tyzoon K, Alessi Dario R, Gray Nathanael S
Abstract excerpt
Mutations in leucine-rich repeat kinase 2 (LRRK2) are strongly associated with late-onset autosomal dominant Parkinson's disease. We employed a new, 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 and Ser935 and accumulation of LRRK2 within aggregate structures. LRRK2-IN-1 will serve...
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