Article
Selective Inhibitors of G2019S-LRRK2 Kinase Activity.
Journal of medicinal chemistry - 10 Dec 2020
Garofalo Albert W, Bright Jessica, De Lombaert Stéphane, Toda Alyssa M A, Zobel Kerry, Andreotti Daniele, Beato Claudia, Bernardi Silvia, Budassi Federica, Caberlotto Laura, Gao Peng, Griffante Cristiana, Liu Xinying, Mengatto Luisa, Migliore Marco, Sabbatini Fabio Maria, Sava Anna, Serra Elena, Vincetti Paolo, Zhang Mingliang, Carlisle Holly J
Abstract excerpt
Pathogenic variants in the leucine-rich repeat kinase 2 (LRRK2) gene have been identified that increase the risk for developing Parkinson's disease in a dominantly inherited fashion. These pathogenic variants, of which G2019S is the most common, cause abnormally high kinase activity, and compounds that inhibit this activity are being pursued as potentially disease-modifying therapeutics. Because LRRK2 regulates...
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