After the discovery of leucine-rich repeat kinase 2 (LRRK2) as a risk factor for sporadic Parkinson's disease (PD) and mutations in LRRK2 as a cause of some forms of familial PD, there has been substantial interest in finding chemical modulators of LRRK2 function. Most of the pathogenic mutations in LRRK2 are within the enzymatic cores of the protein; therefore, many screens have focused on finding chemical modulators of this enzymatic activity. There are alternative screening approaches that could be taken to investigate compounds that modulate LRRK2 cellular functions. These screens are more often phenotypic screens. The preparation for a screen has to be rigorous and enable high-throughput accurate assessment of a compound's activity. The pipeline to beginning a drug screen and some LRRK2 inhibitor and phenotypic screens will be discussed.
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December 2016
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Views of the Fc region of human immunoglobulin A (IgA) with interaction sites for key host receptors highlighted in the upper images, and those for bacterial IgA binding proteins in the lower ones. The remarkable co-localisation of these sites illustrates how various bacterial pathogens have co-opted sites on immunoglobulins as an effective means to block the elimination mechanisms which immunoglobulins normally trigger. See pp. 1651–1658 for further information. Image provided by J. Woof.
Review Article|
December 02 2016
Screening for chemical modulators for LRRK2
Heather Mortiboys
Heather Mortiboys
SITraN, Neuroscience, University of Sheffield, 385a Glossop Road, Sheffield S10 2HQ, U.K.
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Publisher: Portland Press Ltd
Received:
August 12 2016
Revision Received:
August 25 2016
Accepted:
September 29 2016
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2016 The Author(s); published by Portland Press Limited on behalf of the Biochemical Society
2016
Biochem Soc Trans (2016) 44 (6): 1617–1623.
Article history
Received:
August 12 2016
Revision Received:
August 25 2016
Accepted:
September 29 2016
Citation
Heather Mortiboys; Screening for chemical modulators for LRRK2. Biochem Soc Trans 15 December 2016; 44 (6): 1617–1623. doi: https://doi.org/10.1042/BST20160242
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