Screening for chemical modulators for LRRK2.

Abstract:

: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.

journal_name

Biochem Soc Trans

authors

Mortiboys H

doi

10.1042/BST20160242

subject

Has Abstract

pub_date

2016-12-15 00:00:00

pages

1617-1623

issue

6

eissn

0300-5127

issn

1470-8752

pii

BST20160242

journal_volume

44

pub_type

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