LRRK2

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. 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.

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  • GSK 2578215A
    2181
    GSK 2578215A
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    From $137.50

  • GNE 7915
    2348
    GNE 7915
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  • LRRK2-IN-1
    2493
    LRRK2-IN-1
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  • PF 06447475
    2546
    PF 06447475
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  • RN277
    4400
    RN277
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    From $143.00

5 Items

More About 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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