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Table 2 LRRK2 as a therapeutic target for parkinsonism

From: The role of the LRRK2 gene in Parkinsonism

   Model systems Possible outcome Clinical results
Kinase inhibitor Staurosporine both in vitro and in vivo Inhibits LRRK2 autophosphorylation or LRRK2-mediated phosphorylation of myelin basic protein. Disrupts LRRK2 dimers. -
Sunitinib in vitro Inhibits LRRK2-mediated phosphorylation of LRRKtide and Nictide. The LRRK2 A2016T mutant is resistant to this compound. -
H-1152 in vitro Inhibits LRRK2-mediated phosphorylation of LRRKtide and Nictide. The LRRK2 A2017T mutant is resistant to this compound. -
Indirubin-3’-monooxime both in vitro and in vivo Inhibits LRRK2 autophosphorylation and MBP and 4E-BP phosphorylation. -
Sorafenib C. elegans and Drosophila models Inhibits LRRK2 autophosphorylation and LRRK2-mediated MBP phosphorylation. -
GW5074 C. elegans and Drosophila models Inhibits LRRK2 autophosphorylation and MBP and 4E-BP phosphorylation. -
CZC-25146 rodent model Inhibits mutant LRRK2-mediated toxicity in primary rodent and human neurons. -
CZC-54252 rodent model Inhibits mutant LRRK2-mediated toxicity in human neurons. -
LRRK2-IN-1 rodent model Induces loss of 14-3-3 binding to LRRK2. Promotes dephosphorylation of Ser910 and Ser935 on LRRK2. -
GTPase modulator ArfGAP1 Drosophila model Enhances both WT and mutant LRRK2 GTP hydrolysis. -
Synthetic agent diapocynin rodent model - protect neurobehavioral function