nvp-tae684 and Parkinson-Disease

nvp-tae684 has been researched along with Parkinson-Disease* in 1 studies

Other Studies

1 other study(ies) available for nvp-tae684 and Parkinson-Disease

Article	Year
Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorganic & medicinal chemistry letters, 2012, Mar-01, Volume: 22, Issue:5 Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3μM in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10mg/kg. Topics: Animals; Brain; Cell Line; Cells, Cultured; Humans; Leucine-Rich Repeat Serine-Threonine Protein Kinase-2; Mice; Models, Molecular; Mutation; Parkinson Disease; Protein Serine-Threonine Kinases; Pyrimidines	2012

Article

Year

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

Bioorganic & medicinal chemistry letters, 2012, Mar-01, Volume: 22, Issue:5

Leucine-rich repeat kinase 2 (LRRK2) is linked to Parkinson's disease and may represent an attractive therapeutic target. Here we report a 2,4-dianilino-5-chloro-pyrimidine, TAE684, a previously reported inhibitor of anaplastic lymphoma kinase (ALK), is also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3μM in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10mg/kg.

Topics: Animals; Brain; Cell Line; Cells, Cultured; Humans; Leucine-Rich Repeat Serine-Threonine Protein Kinase-2; Mice; Models, Molecular; Mutation; Parkinson Disease; Protein Serine-Threonine Kinases; Pyrimidines

2012