Inhibitors of Leucine-Rich Repeat Kinase 2 (LRRK2): Progress and Promise for the Treatment of Parkinson's Disease

被引:16
|
作者
Gilligan, Paul J. [1 ]
机构
[1] Penn Drug Discovery Inst, Doylestown, PA 18902 USA
关键词
Kinase inhibitors; Leucine-rich repeat kinase 2 (LRRK2); Parkinson's disease; ALPHA-SYNUCLEIN; GENE; MUTATIONS; G2019S; POTENT; DISCOVERY; PHOSPHORYLATION; EXPRESSION; FAMILIES; MODEL;
D O I
10.2174/156802661510150328223655
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Mutations in the gene for leucine-rich repeat kinase 2 (LRRK2) have been linked to several familial and sporadic late-onset cases of Parkinson's disease. The cumulative data for the effects of mutant forms of this enzyme on neuronal degradation and the pathophysiology of Parkinson's disease create a compelling case for drug discovery based on inhibition of the mutant forms of LRRK2. This review focuses on structure-activity relationships for inhibitors of LRRK2 and the data supporting a potential role of these agents in treating Parkinson's disease.
引用
收藏
页码:927 / 938
页数:12
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