LRRK2

Leucine-rich repeat kinase 2 (LRRK2; EC 2.7.11.1) is a promising therapeutic target for some forms of Parkinson’s disease. because of a missense mutation, G2019S, that is frequently found not only in familial but also sporadic Parkinson’s disease cases. The LRRK2 G2019S mutation enhances kinase activity, suggesting that small molecule inhibitors may be able to block aberrant LRRK2-dependent signaling in Parkinson’s disease[1]. However, the physiological function of LRRK2 kinase as well as its endogenous protein substrates remains poorly understood. There have been several papers describing potential cellular substrates as well as endogenous functions for this complex protein in the mammalian neuron. Potential substrates include ezrin, radixin moesin (ERM) proteins, mitogen-activated protein kinase (MAPK), eukaryotic initiation factor 4E (eIF4E)-binding protein (4E-BP), futsch, autophosphorylation, and 14-3-3 proteins[2].


[1] A.D. Reith et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg. Med. Chem. Lett. 2012, 22, 5625-5629.
[2] R.E. Drolet et al. Leucine-rich repeat kinase 2 (LRRK2) cellular biology: a review of recent advances in identifying physiological substrates and cellular functions. J. Neurogenet. 2011, 25, 140-151.

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Axon ID Name Description From price
2546 PF 06447475 Potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor €85.00
2493 LRRK2-IN-1 Potent, ATP-competitive and selective inhibitor of LRRK2 €85.00
2181 GSK 2578215A Potent and highly selective LRRK2 inhibitor €125.00
2348 GNE 7915 Potent, selective, metabolically stable, and brain-penetrable LRRK2 inhibitor €110.00

4 Item(s)

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