Small-Molecule Inhibitors of LRRK2

John M. Hatcher, Hwan Geun Choi, Dario R. Alessi, Nathanael S. Gray (Lead / Corresponding author)

Research output: Chapter in Book/Report/Conference proceedingChapter (peer-reviewed)

14 Citations (Scopus)

Abstract

Mutations in the leucine-rich repeat kinase 2 (LRRK2) protein have been genetically and functionally linked to Parkinson's disease (PD). The kinase activity of LRRK2 is increased by pathogenic mutations; therefore, modulation of LRRK2 kinase activity by a selective small-molecule inhibitor has been proposed as a potentially viable treatment for Parkinson's disease. This chapter presents a historical overview of the development and bioactivity of several small-molecule LRRK2 inhibitors that have been used to inhibit LRRK2 kinase activity in vitro or in vivo. These compounds are important tools for understanding the cellular biology of LRRK2 and for evaluating the potential of LRRK2 inhibitors as disease-modifying PD therapies.

Original languageEnglish
Title of host publicationLeucine-Rich Repeat Kinase 2 (LRRK2)
EditorsHardy J. Rideout
PublisherSpringer International Publishing
Pages241-264
Number of pages24
ISBN (Electronic)9783319499697
ISBN (Print)9783319499673
DOIs
Publication statusPublished - 2017

Publication series

NameAdvances in neurobiology
PublisherSpringer International Publishing
Volume14
ISSN (Print)2190-5215

Keywords

  • Parkinson’s disease
  • Leucine-rich repeat kinase 2 (LRRK2)
  • LRRK2 inhibitors
  • Mutations

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    Hatcher, J. M., Choi, H. G., Alessi, D. R., & Gray, N. S. (2017). Small-Molecule Inhibitors of LRRK2. In H. J. Rideout (Ed.), Leucine-Rich Repeat Kinase 2 (LRRK2) (pp. 241-264). (Advances in neurobiology; Vol. 14). Springer International Publishing. https://doi.org/10.1007/978-3-319-49969-7_13