Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2 Academic Article uri icon

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abstract

  • Mutations in leucine-rich repeat kinase 2 (LRRK2) are strongly associated with late-onset autosomal dominant Parkinson's disease. We employed a new, parallel, compound-centric approach to identify a potent and selective LRRK2 inhibitor, LRRK2-IN-1, and demonstrated that inhibition of LRRK2 induces dephosphorylation of Ser910 and Ser935 and accumulation of LRRK2 within aggregate structures. LRRK2-IN-1 will serve as a versatile tool to pharmacologically interrogate LRRK2 biology and study its role in Parkinson's disease.

authors

  • Steinberg, Gregory
  • Deng, Xianming
  • Dzamko, Nicolas
  • Prescott, Alan
  • Davies, Paul
  • Liu, Qingsong
  • Yang, Qingkai
  • Lee, Jiing-Dwan
  • Patricelli, Matthew P
  • Nomanbhoy, Tyzoon K
  • Alessi, Dario R
  • Gray, Nathanael S

publication date

  • April 2011

has subject area