Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors

No abstract is available for this paper.

• Publication year

  2014

• Venue

  Unknown venue

• Publication date

  Unknown publication date

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1007/7355_2014_69
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

• The Parkinson Disease-linked LRRK2 Protein Mutation I2020T Stabilizes an Active State Conformation Leading to Increased Kinase Activity*

  2014influential reference
• Unbiased screen for interactors of leucine-rich repeat kinase 2 supports a common pathway for sporadic and familial Parkinson disease

  2014cited by this paper
• Surfactant Secretion in LRRK2 Knock-Out Rats: Changes in Lamellar Body Morphology and Rate of Exocytosis

  2014cited by this paper
• LRRK2 and neuroinflammation: partners in crime in Parkinson’s disease?

  2014cited by this paper
• Leucine-Rich Repeat Kinase 2 Binds to Neuronal Vesicles through Protein Interactions Mediated by Its C-Terminal WD40 Domain

  2014cited by this paper
• Ribosomal protein s15 phosphorylation mediates LRRK2 neurodegeneration in Parkinson's disease.

  2014cited by this paper
• Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

  2014influential reference
• Membrane recruitment of endogenous LRRK2 precedes its potent regulation of autophagy.

  2014cited by this paper
• ERKed by LRRK2: a cell biological perspective on hereditary and sporadic Parkinson's disease.

  2014cited by this paper
• Phosphoproteomic evaluation of pharmacological inhibition of leucine‐rich repeat kinase 2 reveals significant off‐target effects of LRRK‐2‐IN‐1

  2014cited by this paper
• Association Studies of Sporadic Parkinson’s Disease in the Genomic Era

  2014cited by this paper
• Ageing and Parkinson's disease: Why is advancing age the biggest risk factor?☆

  2014cited by this paper
• Novel cinnoline-based inhibitors of LRRK2 kinase activity.

  2013cited by this paper
• The hallmarks of Parkinson's disease

  2013cited by this paper
• Type II kinase inhibitors show an unexpected inhibition mode against Parkinson's disease-linked LRRK2 mutant G2019S.

  2013influential reference
• Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones

  2013cited by this paper
• The impact of reactive oxygen species and genetic mitochondrial mutations in Parkinson's disease.

  2013cited by this paper
• Differential effects of familial parkinson mutations in LRRK2 revealed by a systematic analysis of autophosphorylation.

  2013cited by this paper
• LRRK2 phosphorylates novel tau epitopes and promotes tauopathy

  2013cited by this paper
• Triazolopyridazine LRRK2 kinase inhibitors.

  2013cited by this paper
• Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

  2013cited by this paper
• Contribution of GTPase activity to LRRK2-associated Parkinson disease

  2013cited by this paper
• LRRK2 phosphorylates Snapin and inhibits interaction of Snapin with SNAP-25

  2013cited by this paper
• LRRK2: Cause, Risk, and Mechanism

  2013cited by this paper
• GTPase activity regulates kinase activity and cellular phenotypes of Parkinson's disease-associated LRRK2.

  2013cited by this paper
• The Neurobiology of LRRK2 and its Role in the Pathogenesis of Parkinson’s Disease

  2013cited by this paper
• Leucine-Rich Repeat Kinase 2 (LRRK2)-Deficient Rats Exhibit Renal Tubule Injury and Perturbations in Metabolic and Immunological Homeostasis

  2013cited by this paper
• Dysfunction of the autophagy/lysosomal degradation pathway is a shared feature of the genetic synucleinopathies

  2013cited by this paper
• Comprehensive characterization and optimization of anti-LRRK2 (leucine-rich repeat kinase 2) monoclonal antibodies

  2013cited by this paper
• Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.

  2013cited by this paper
• Kinase inhibitors arrest neurodegeneration in cell and C. elegans models of LRRK2 toxicity.

  2013cited by this paper
• The genetics of Parkinson's disease: Progress and therapeutic implications

  2013influential reference
• Activities at the Universal Protein Resource (UniProt)

  2013cited by this paper
• MicroRNA-205 regulates the expression of Parkinson's disease-related leucine-rich repeat kinase 2 protein.

  2013cited by this paper
• Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.

  2013cited by this paper
• Loss of Leucine-Rich Repeat Kinase 2 (LRRK2) in Rats Leads to Progressive Abnormal Phenotypes in Peripheral Organs

  2013cited by this paper
• Commentary: Progressive inflammation as a contributing factor to early development of Parkinson's disease.

  2013cited by this paper
• Spread of neuronal degeneration in a dopaminergic, Lrrk-G2019S model of Parkinson disease

  2013cited by this paper
• LRRK2 as a Potential Genetic Modifier of Synucleinopathies: Interlacing the Two Major Genetic Factors of Parkinson's Disease

  2013cited by this paper
• 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?

  2013cited by this paper
• Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

  2012influential reference
• Biochemical Characterization of Highly Purified Leucine-Rich Repeat Kinases 1 and 2 Demonstrates Formation of Homodimers

  2012cited by this paper
• Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

  2012influential reference
• ArfGAP1 Is a GTPase Activating Protein for LRRK2: Reciprocal Regulation of ArfGAP1 by LRRK2

  2012cited by this paper
• Phosphorylation of 4E-BP1 in the Mammalian Brain Is Not Altered by LRRK2 Expression or Pathogenic Mutations

  2012cited by this paper
• GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.

  2012cited by this paper
• LRRK2 Inhibition Attenuates Microglial Inflammatory Responses

  2012cited by this paper
• LRRK2 GTPase dysfunction in the pathogenesis of Parkinson's disease.

  2012cited by this paper
• GTPase Activity and Neuronal Toxicity of Parkinson's Disease–Associated LRRK2 Is Regulated by ArfGAP1

  2012cited by this paper
• LRRK2 Phosphorylates Tubulin-Associated Tau but Not the Free Molecule: LRRK2-Mediated Regulation of the Tau-Tubulin Association and Neurite Outgrowth

  2012cited by this paper
• Analysis of LRRK2 accessory repeat domains: prediction of repeat length, number and sites of Parkinson's disease mutations.

  2012influential reference
• LRRK2 interactions with α-synuclein in Parkinson’s disease brains and in cell models

  2012cited by this paper
• (G2019S) LRRK2 activates MKK4-JNK pathway and causes degeneration of SN dopaminergic neurons in a transgenic mouse model of PD

  2012cited by this paper
• Characterization of TAE684 as a potent LRRK2 kinase inhibitor.

  2012cited by this paper
• Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations

  2012cited by this paper
• LRRK2 controls an EndoA phosphorylation cycle in synaptic endocytosis.

  2012cited by this paper
• Brain Penetrant LRRK2 Inhibitor.

  2012cited by this paper
• Ser1292 Autophosphorylation Is an Indicator of LRRK2 Kinase Activity and Contributes to the Cellular Effects of PD Mutations

  2012influential reference
• Number and brightness analysis of LRRK2 oligomerization in live cells.

  2012cited by this paper
• Current understanding of LRRK2 in Parkinson's disease: biochemical and structural features and inhibitor design.

  2012influential reference
• LRRK2 haplotype‐sharing analysis in Parkinson's disease reveals a novel p.S1761R mutation

  2012cited by this paper
• The GTPase function of LRRK2.

  2012cited by this paper
• Expression, purification and preliminary biochemical and structural characterization of the leucine rich repeat namesake domain of leucine rich repeat kinase 2.

  2012cited by this paper
• Too many roads not taken

  2011cited by this paper
• Characterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2

  2011cited by this paper
• Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons.

  2011cited by this paper
• Development of a new permeability assay using low-efflux MDCKII cells.

  2011cited by this paper
• LRRK2 Kinase Activity Is Dependent on LRRK2 GTP Binding Capacity but Independent of LRRK2 GTP Binding

  2011cited by this paper
• LRRK2 protein levels are determined by kinase function and are crucial for kidney and lung homeostasis in mice

  2011cited by this paper
• Kinetic, mechanistic, and structural modeling studies of truncated wild-type leucine-rich repeat kinase 2 and the G2019S mutant.

  2011cited by this paper
• Autophosphorylation in the leucine-rich repeat kinase 2 (LRRK2) GTPase domain modifies kinase and GTP-binding activities.

  2011cited by this paper
• Identification of chemicals to inhibit the kinase activity of leucine-rich repeat kinase 2 (LRRK2), a Parkinson's disease-associated protein.

  2011cited by this paper
• LRRK2 directly phosphorylates Akt1 as a possible physiological substrate: Impairment of the kinase activity by Parkinson's disease‐associated mutations

  2011cited by this paper
• Comprehensive analysis of kinase inhibitor selectivity

  2011cited by this paper
• Genetic characteristics of leucine-rich repeat kinase 2 (LRRK2) associated Parkinson's disease.

  2011cited by this paper
• Structure and function of WD40 domain proteins

  2011cited by this paper
• A Rat Model of Progressive Nigral Neurodegeneration Induced by the Parkinson's Disease-Associated G2019S Mutation in LRRK2

  2011cited by this paper
• Insight into the mode of action of the LRRK2 Y1699C pathogenic mutant

  2011cited by this paper
• Temporal Expression of Mutant LRRK2 in Adult Rats Impairs Dopamine Reuptake

  2011cited by this paper
• A guide to neurotoxic animal models of Parkinson's disease.

  2011cited by this paper
• Dopaminergic Neuronal Loss, Reduced Neurite Complexity and Autophagic Abnormalities in Transgenic Mice Expressing G2019S Mutant LRRK2

  2011cited by this paper
• LRRK2 signaling pathways: the key to unlocking neurodegeneration?

  2011cited by this paper
• Leucine-Rich Repeat Kinase 2 (LRRK2) Cellular Biology: A Review of Recent Advances in Identifying Physiological Substrates and Cellular Functions

  2011cited by this paper
• The role of leucine-rich repeat kinase 2 (LRRK2) in Parkinson's disease

  2010cited by this paper
• Signal Transduction Protein Array Analysis Links LRRK2 to Ste20 Kinases and PKC Zeta That Modulate Neuronal Plasticity

  2010cited by this paper
• 14-3-3 binding to LRRK2 is disrupted by multiple Parkinson's disease-associated mutations and regulates cytoplasmic localization

  2010cited by this paper
• Activation of FoxO by LRRK2 induces expression of proapoptotic proteins and alters survival of postmitotic dopaminergic neuron in Drosophila.

  2010cited by this paper
• The Parkinson's Disease Associated LRRK2 Exhibits Weaker In Vitro Phosphorylation of 4E-BP Compared to Autophosphorylation

  2010cited by this paper
• Enhanced Striatal Dopamine Transmission and Motor Performance with LRRK2 Overexpression in Mice Is Eliminated by Familial Parkinson's Disease Mutation G2019S

  2010cited by this paper
• Inhibitors of Leucine Rich Repeat Kinase 2 (LRRK2) Protect Against LRRK2-Models of Parkinson’s Disease

  2010cited by this paper
• MKK6 binds and regulates expression of Parkinson’s disease‐related protein LRRK2

  2010cited by this paper
• Development of a mechanism-based high-throughput screen assay for leucine-rich repeat kinase 2--discovery of LRRK2 inhibitors.

  2010cited by this paper
• LRRK2 Is Involved in the IFN-γ Response and Host Response to Pathogens

  2010cited by this paper
• Inhibition of LRRK2 kinase activity leads to dephosphorylation of Ser910/Ser935, disruption of 14-3-3 binding and altered cytoplasmic localization

  2010cited by this paper
• Membrane localization of LRRK2 is associated with increased formation of the highly active LRRK2 dimer and changes in its phosphorylation.

  2010cited by this paper
• Identification and Characterization of a Leucine-Rich Repeat Kinase 2 (LRRK2) Consensus Phosphorylation Motif

  2010influential reference
• Loss of leucine-rich repeat kinase 2 causes impairment of protein degradation pathways, accumulation of α-synuclein, and apoptotic cell death in aged mice

  2010cited by this paper
• Phosphopeptide analysis reveals two discrete clusters of phosphorylation in the N-terminus and the Roc domain of the Parkinson-disease associated protein kinase LRRK2.

  2010cited by this paper
• Armadillo-repeat protein functions: questions for little creatures.

  2010cited by this paper
• Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties.

  2010cited by this paper

• Modeling Parkinson’s disease in LRRK2 rodents

  2023cites this paper
• Constitutive silencing of LRRK2 kinase activity leads to early glucocerebrosidase deregulation and late impairment of autophagy in vivo.

  2021cites this paper
• Leucine-rich repeat kinase 2 inhibitors: a patent review (2014-2016)

  2017cites this paper
• Regulation of LRRK2 by Phosphatases.

  2017cites this paper
• LRRK2 Kinase Inhibition as a Therapeutic Strategy for Parkinson’s Disease, Where Do We Stand?

  2016cites this paper
• Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.

  2015cites this paper