In silico, in vitro and cellular analysis with a kinome-wide inhibitor panel correlates cellular LRRK2 dephosphorylation to inhibitor activity on LRRK2. (Q40188432)

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scientific article published on 3 June 2014

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English	In silico, in vitro and cellular analysis with a kinome-wide inhibitor panel correlates cellular LRRK2 dephosphorylation to inhibitor activity on LRRK2.	scientific article published on 3 June 2014

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20 March 2020

In silico, in vitro and cellular analysis with a kinome-wide inhibitor panel correlates cellular LRRK2 dephosphorylation to inhibitor activity on LRRK2 (English)

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20 March 2020

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20 March 2020

Jean-Marc Taymans

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20 March 2020

Veerle Baekelandt

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Veerle Baekelandt

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20 March 2020

Renée Vancraenenbroeck

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Renée Vancraenenbroeck

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20 March 2020

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Joren De Raeymaecker

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20 March 2020

Fangye Gao

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20 March 2020

Marc De Maeyer

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20 March 2020

Frontiers in Molecular Neuroscience

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20 March 2020

Identification of protein phosphatase 1 as a regulator of the LRRK2 phosphorylation cycle

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The genetics of Parkinson's disease: progress and therapeutic implications

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Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).

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Brain Penetrant LRRK2 Inhibitor

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22 September 2017

Kinase inhibitors arrest neurodegeneration in cell and C. elegans models of LRRK2 toxicity

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22 September 2017

Phosphorylation of LRRK2: from kinase to substrate

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22 September 2017

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22 September 2017

Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation

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GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

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Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models.

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22 September 2017

The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling

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22 September 2017

The G2385R variant of leucine-rich repeat kinase 2 associated with Parkinson's disease is a partial loss-of-function mutation

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Leucine-rich repeat kinase 2 (LRRK2) as a potential therapeutic target in Parkinson's disease

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Characterization of TAE684 as a potent LRRK2 kinase inhibitor

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22 September 2017

Phosphorylation of LRRK2 serines 955 and 973 is disrupted by Parkinson's disease mutations and LRRK2 pharmacological inhibition

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22 September 2017

LRRK2 kinase activity is dependent on LRRK2 GTP binding capacity but independent of LRRK2 GTP binding

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Kinases as targets for Parkinson's disease: from genetics to therapy

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22 September 2017

Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein

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22 September 2017

Phosphorylation-dependent 14-3-3 binding to LRRK2 is impaired by common mutations of familial Parkinson's disease

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22 September 2017

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.

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22 September 2017

The role of leucine-rich repeat kinase 2 (LRRK2) in Parkinson's disease

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22 September 2017

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

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22 September 2017

Inhibitors of leucine-rich repeat kinase-2 protect against models of Parkinson's disease

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22 September 2017

Inhibition of LRRK2 kinase activity leads to dephosphorylation of Ser(910)/Ser(935), disruption of 14-3-3 binding and altered cytoplasmic localization

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22 September 2017

14-3-3 binding to LRRK2 is disrupted by multiple Parkinson's disease-associated mutations and regulates cytoplasmic localization

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Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease

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22 September 2017

The Parkinson's disease kinase LRRK2 autophosphorylates its GTPase domain at multiple sites

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Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models

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22 September 2017

Knowledge based prediction of ligand binding modes and rational inhibitor design for kinase drug discovery

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22 September 2017

Phenotype, genotype, and worldwide genetic penetrance of LRRK2-associated Parkinson's disease: a case-control study

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22 September 2017

Kinase signaling pathways as potential targets in the treatment of Parkinson's disease

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The selectivity of protein kinase inhibitors: a further update

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22 September 2017

LRRK2 phosphorylates moesin at threonine-558: characterization of how Parkinson's disease mutants affect kinase activity

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Parkinson's disease-associated mutations in LRRK2 link enhanced GTP-binding and kinase activities to neuronal toxicity

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Kinase activity of mutant LRRK2 mediates neuronal toxicity

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22 September 2017

Kinase activity is required for the toxic effects of mutant LRRK2/dardarin

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22 September 2017

LRRK2 in Parkinson's disease: protein domains and functional insights

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The conformational plasticity of protein kinases

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17 June 2018

ATP-competitive LRRK2 inhibitors interfere with monoclonal antibody binding to the kinase domain of LRRK2 under native conditions. A method to directly monitor the active conformation of LRRK2?

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17 June 2018

Development of an enzyme-linked immunosorbent assay for detection of cellular and in vivo LRRK2 S935 phosphorylation

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LRRK2 and human disease: a complicated question or a question of complexes?

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Phosphopeptide analysis reveals two discrete clusters of phosphorylation in the N-terminus and the Roc domain of the Parkinson-disease associated protein kinase LRRK2.

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Determination of a large number of kinase activities using peptide substrates, P81 phosphocellulose paper arrays and phosphor imaging.

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The Parkinson disease gene LRRK2: evolutionary and structural insights

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12 December 2020

based on heuristic

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Comprehensive analysis of LRRK2 in publicly available Parkinson's disease cases and neurologically normal controls

1 reference

https://pubmed.ncbi.nlm.nih.gov/24917786

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo

1 reference

https://pubmed.ncbi.nlm.nih.gov/24917786

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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10.3389/FNMOL.2014.00051

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20 March 2020

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20 March 2020

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20 March 2020

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