PubMed:23066449 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PubMed/sourceid/23066449","sourcedb":"PubMed","sourceid":"23066449","source_url":"https://www.ncbi.nlm.nih.gov/pubmed/23066449","text":"Brain Penetrant LRRK2 Inhibitor.\nActivating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here we report a 2-anilino-4-methylamino-5-chloropyrimidine, HG-10-102-01(4) is a potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant. Compound 4 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 µM in cells and is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.","tracks":[]}