title: Inhibitors of leucine-rich repeat kinase 2 (LRRK2): progress and promise for the treatment of 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.
authors.affiliation: The Pennsylvania Drug Discovery Institute, 3805 Old Easton Road, Doylestown, PA 18902, USA. pjgillig@gmail.com.
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
mesh_terms: D000818:Animals; D006801:Humans; D000071158:Leucine-Rich Repeat Serine-Threonine Protein Kinase-2; D010300:Parkinson Disease / Q000188:drug therapy* / Q000201:enzymology*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D047428:Protein Kinase Inhibitors; C495280:LRRK2 protein, human; D000071158:Leucine-Rich Repeat Serine-Threonine Protein Kinase-2; C495279:Lrrk2 protein, mouse; D017346:Protein Serine-Threonine Kinases