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Article

Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.

European journal of medicinal chemistry - 15 Nov 2022

Leśniak Robert K, Nichols R Jeremy, Schonemann Marcus, Zhao Jing, Gajera Chandresh R, Lam Grace, Nguyen Khanh C, Langston J William, Smith Mark, Montine Thomas J

Abstract excerpt

Mutations in the Leucine Rich Repeat Protein Kinase 2 gene (LRRK2) are genetic predispositions for Parkinson's Disease, of which the G2019S (GS) missense mutation is the most common. GS-LRRK2 has a hyperactive kinase, and although numerous drug discovery programs have targeted the LRRK2 kinase, few have reached clinical trials. We recently reported on the discovery of a novel LRRK2 kinase inhibitor chemotype,...

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PMID: 36049274
DOI: 10.1016/j.ejmech.2022.114693

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