Article
Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy.
European journal of medicinal chemistry - 5 Feb 2022
Leśniak Robert K, Nichols R Jeremy, Schonemann Marcus, Zhao Jing, Gajera Chandresh R, Fitch William L, Lam Grace, Nguyen Khanh C, Smith Mark, Montine Thomas J
Abstract excerpt
Mutations in the Leucine Rich Repeat Protein Kinase 2 gene (LRRK2) are the most common genetic causes of Parkinson's Disease (PD). The G2019S mutation is the most common inherited LRRK2 mutation, occurs in the kinase domain, and results in increased kinase activity. We report the discovery and development of compound 38, an indazole-based, G2019S-selective (>2000-fold vs. WT) LRRK2 inhibitor capable of entering...
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