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

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2015年 / 15卷 / 10期

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

页码：927 / 938

页数：12

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