期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 14, 页码 4085-4090出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.054
关键词
Leucine-rich repeat kinase 2; LRRK2; LRRK2 inhibitors; Kinase inhibitors; Parkinson's disease
Mutations in leucine-rich repeat kinase-2 (LRRK2) are the most common genetic cause of Parkinson's disease (PD). The most frequent kinase-enhancing mutation is the G2019S residing in the kinase activation domain. This opens up a promising therapeutic avenue for drug discovery targeting the kinase activity of LRRK2 in PD. Several LRRK2 inhibitors have been reported to date. Here, we report a selective, brain penetrant LRRK2 inhibitor and demonstrate by a competition pulldown assay in vivo target engagement in mice. (C) 2013 Elsevier Ltd. All rights reserved.
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