This week in techniques



Licensing status

Publication and contact information

Assays & screens

Assays to monitor leucine-rich repeat kinase 2 (LRRK2) activity

Cell-based and pharmacodynamic assays for monitoring LRRK2 activity could help identify compounds to treat Parkinson's disease (PD). The assays were designed to detect autophosphorylation at the Ser1291 residue of the LRRK2 protein, which has been linked to PD. In a screening study using the assays, the diaminopyrimidine-based compound G1023 was identified as an inhibitor of LRRK2 autophosphorylation with an IC50 value below 10 nM. In hippocampal neurons from mice carrying PD-associated mutations in Lrrk2, G1023 decreased neurite outgrowth defects compared with vehicle control. Next steps include studies to determine whether blocking LRRK2 activity in mice could reverse the onset and progression of PD.

SciBX 6(1); doi:10.1038/scibx.2013.22
Published online Jan. 10, 2013

Patent applications filed; licensing status undisclosed

Sheng, Z. et al. Sci. Transl. Med.; published online Dec. 12, 2012;
Contact: Haitao Zhu, Genentech Inc., South San Francisco, Calif.

Contact: Donald S. Kirkpatrick, same affiliation as above