Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons.

@article{Ramsden2011ChemoproteomicsbasedDO,
  title={Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons.},
  author={Nigel Ramsden and Jessica Marie Liliane Perrin and Zhao Hua Ren and Byoung Dae Lee and N. D. Zinn and Valina L. Dawson and Danny W H Tam and Michael P. Bova and Manja Lang and G. W. J. Drewes and Marcus Bantscheff and Fr{\'e}d{\'e}rique Bard and Ted M. Dawson and Carsten Hopf},
  journal={ACS chemical biology},
  year={2011},
  volume={6 10},
  pages={
          1021-8
        }
}
Leucine-rich repeat kinase-2 (LRRK2) mutations are the most important cause of familial Parkinson's disease, and non-selective inhibitors are protective in rodent disease models. Because of their poor potency and selectivity, the neuroprotective mechanism of these tool compounds has remained elusive so far, and it is still unknown whether selective LRRK2 inhibition can attenuate mutant LRRK2-dependent toxicity in human neurons. Here, we employ a chemoproteomics strategy to identify potent… CONTINUE READING
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