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Nat Chem Biol. 2011 Apr;7(4):203-5. doi: 10.1038/nchembio.538. Epub 2011 Mar 6.

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.

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  • 1Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, Massachusetts, USA.

Abstract

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 as a versatile tool to pharmacologically interrogate LRRK2 biology and study its role in Parkinson's disease.

PMID:
21378983
[PubMed - indexed for MEDLINE]
PMCID:
PMC3287420
Free PMC Article
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