Selective, Brain-Penetrant Small Molecule Inhibitors of LRRK2: A Discovery Story

Upregulation of LRRK2 expression has been identified as a disease driver in a subset of Parkinson's disease patients, making inhibition of this kinase an attractive target in the search for treatment options.

In this webinar, we review a successful small molecule drug discovery project conducted by a team of scientists from Genentech and Charles River that spanned hit identification and lead optimization of a highly potent LRRK2 inhibitor. Approaches to compound-related challenges, including the requirement for selectivity over other structurally-related kinases and ensuring blood-brain barrier permeability will be discussed.

Presenter

  • Charles Baker-Glenn, DPhil, Team Leader, Charles River