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

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

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

http://www.wikidata.org/entity/Q34398451

about

LRRK2 kinase activity regulates synaptic vesicle trafficking and neurotransmitter release through modulation of LRRK2 macro-molecular complex Dysregulation of lysosomal morphology by pathogenic LRRK2 is corrected by TPC2 inhibition Activation Mechanism of LRRK2 and Its Cellular Functions in Parkinson's Disease Ten years and counting: moving leucine-rich repeat kinase 2 inhibitors to the clinic LRRK2 G2019S mutation attenuates microglial motility by inhibiting focal adhesion kinase.LRRK2 inhibitors and their potential in the treatment of Parkinson's disease: current perspectives Inhibition of LRRK2 kinase activity stimulates macroautophagy Phosphoproteomics reveals that Parkinson's disease kinase LRRK2 regulates a subset of Rab GTPases 'Up with the LRRK': a phosphorylated Rab10 assay for evaluation of LRRK2 activity and inhibitor engagement mTOR independent regulation of macroautophagy by Leucine Rich Repeat Kinase 2 via Beclin-1 Membrane recruitment of endogenous LRRK2 precedes its potent regulation of autophagy.Kinase drug discovery--what's next in the field?Unique functional and structural properties of the LRRK2 protein ATP-binding pocket.Lack of correlation between the kinase activity of LRRK2 harboring kinase-modifying mutations and its phosphorylation at Ser910, 935, and Ser955.Leucine-rich repeat kinase 2 modulates neuroinflammation and neurotoxicity in models of human immunodeficiency virus 1-associated neurocognitive disorders Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor.The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.Neurite Aggregation and Calcium Dysfunction in iPSC-Derived Sensory Neurons with Parkinson's Disease-Related LRRK2 G2019S Mutation.Phos-tag analysis of Rab10 phosphorylation by LRRK2: a powerful assay for assessing kinase function and inhibitors.Effects of LRRK2 Inhibitors on Nigrostriatal Dopaminergic Neurotransmission Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011).Structural biology of the LRRK2 GTPase and kinase domains: implications for regulation.Leucine-rich repeat kinase 2 inhibitors: a review of recent patents (2011 - 2013).Genetic, structural, and molecular insights into the function of ras of complex proteins domains.Cellular processes associated with LRRK2 function and dysfunction GTP binding regulates cellular localization of Parkinson's disease-associated LRRK2.Leucine-rich repeat kinase 2 and Parkinson's disease.Targeting LRRK2 in Parkinson's disease: an update on recent developments.3D-QSAR and molecular docking study of LRRK2 kinase inhibitors by CoMFA and CoMSIA methods.LRRK2 promotes the activation of NLRC4 inflammasome during Salmonella Typhimurium infection.In silico, in vitro and cellular analysis with a kinome-wide inhibitor panel correlates cellular LRRK2 dephosphorylation to inhibitor activity on LRRK2.Pharmacological LRRK2 kinase inhibition induces LRRK2 protein destabilization and proteasomal degradation Selective LRRK2 kinase inhibition reduces phosphorylation of endogenous Rab10 and Rab12 in human peripheral mononuclear blood cells.LRRK2 dephosphorylation increases its ubiquitination.Phosphoproteomic screening identifies Rab GTPases as novel downstream targets of PINK1.LRRK2 phosphorylates pre-synaptic N-ethylmaleimide sensitive fusion (NSF) protein enhancing its ATPase activity and SNARE complex disassembling rate.Inhibitor treatment of peripheral mononuclear cells from Parkinson's disease patients further validates LRRK2 dephosphorylation as a pharmacodynamic biomarker.Leucine-rich repeat kinase 2 positively regulates inflammation and down-regulates NF-κB p50 signaling in cultured microglia cells.Decreased Sirtuin Deacetylase Activity in LRRK2 G2019S iPSC-Derived Dopaminergic Neurons.Rab10 Phosphorylation Detection by LRRK2 Activity Using SDS-PAGE with a Phosphate-binding Tag.

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

http://www.wikidata.org/entity/Q34398451

description

2012 nî lūn-bûn

@nan

2012 թուականի Յուլիսին հրատարակուած գիտական յօդուած

@hyw

2012 թվականի հուլիսին հրատարակված գիտական հոդված

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2012年の論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年論文

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2012年论文

@wuu

name

GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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type

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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prefLabel

GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

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J.BMCL.2012.06.104

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Bioorganic & Medicinal Chemistry Letters

P1476

GSK2578215A; a potent and high ...... zamide LRRK2 kinase inhibitor.

@en

P2093

Alastair D Reith

http://www.w3.org/2001/XMLSchema#string

Daniele Andreotti

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Hwan Geun Choi

http://www.w3.org/2001/XMLSchema#string

Karamjit Jandu

http://www.w3.org/2001/XMLSchema#string

Lucy Mensah

http://www.w3.org/2001/XMLSchema#string

Nathanael S Gray

http://www.w3.org/2001/XMLSchema#string

Pamela Dossang

http://www.w3.org/2001/XMLSchema#string

Paul Bamborough

http://www.w3.org/2001/XMLSchema#string

Xianming Deng

http://www.w3.org/2001/XMLSchema#string

P2860

The selectivity of protein kinase inhibitors: a further update

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

A small molecule-kinase interaction map for clinical kinase inhibitors

Leucine-rich repeat kinase 2 (LRRK2): a key player in the pathogenesis of Parkinson's disease

Role of LRRK2 kinase dysfunction in Parkinson disease

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

Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

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

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

Leucine-rich repeat kinase 2 mutations and Parkinson's disease: three questions.

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5625-5629

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scholarly article

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10.1016/J.BMCL.2012.06.104

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17

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22

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2012-07-07T00:00:00Z

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230618338

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22863203

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4208292

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