Article
MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.
The Journal of pharmacology and experimental therapeutics - 1 Dec 2015
Fell Matthew J, Mirescu Christian, Basu Kallol, Cheewatrakoolpong Boonlert, DeMong Duane E, Ellis J Michael, Hyde Lynn A, Lin Yinghui, Markgraf Carrie G, Mei Hong, Miller Michael, Poulet Frederique M, Scott Jack D, Smith Michelle D, Yin Zhizhang, Zhou Xiaoping, Parker Eric M, Kennedy Matthew E, Morrow John A
Abstract excerpt
Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are the most common genetic cause of familial and sporadic Parkinson's disease (PD). That the most prevalent mutation, G2019S, leads to increased kinase activity has led to a concerted effort to identify LRRK2 kinase inhibitors as a potential disease-modifying therapy for PD. An internal medicinal chemistry effort identified several potent and highly...
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