MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.

@article{Fell2015MLi2AP,
  title={MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition.},
  author={Matthew J. Fell and Christian Mirescu and Kallol Basu and Boonlert Cheewatrakoolpong and Duane Demong and Jessica M Ellis and Lynn A. Hyde and Yinghui Lin and Carrie G Markgraf and Hong Mei and Michael Miller and Frederique M Poulet and Jack D Scott and Michelle Smith and Zhizhang Yin and Xiaoping Zhou and Eric M. Parker and Matthew E. Kennedy and J Andrew Morrow},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2015},
  volume={355 3},
  pages={397-409}
}
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 selective compounds with favorable drug-like properties. Here, we characterize the… CONTINUE READING
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