Title:Inhibitors of Leucine-Rich Repeat Kinase 2 (LRRK2): Progress and Promise for the Treatment of Parkinson’s Disease
VOLUME: 15 ISSUE: 10
Author(s):Paul J. Gilligan
Affiliation:The Pennsylvania Drug Discovery Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA.
Keywords:Kinase inhibitors, Leucine-rich repeat kinase 2 (LRRK2), Parkinson’s disease.
Abstract: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.