2013
Substrate-Based Fragment Identification for the Development of Selective, Nonpeptidic Inhibitors of Striatal-Enriched Protein Tyrosine Phosphatase
Baguley TD, Xu HC, Chatterjee M, Nairn AC, Lombroso PJ, Ellman JA. Substrate-Based Fragment Identification for the Development of Selective, Nonpeptidic Inhibitors of Striatal-Enriched Protein Tyrosine Phosphatase. Journal Of Medicinal Chemistry 2013, 56: 7636-7650. PMID: 24083656, PMCID: PMC3875168, DOI: 10.1021/jm401037h.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBiphenyl CompoundsBlood-Brain BarrierBoronic AcidsCells, CulturedCerebral CortexHumansNeuronsPermeabilityPhosphorous AcidsProtein Tyrosine Phosphatases, Non-ReceptorRatsRats, Sprague-DawleySmall Molecule LibrariesStereoisomerismStructure-Activity RelationshipSubstrate SpecificityConceptsSubstrate Activity ScreeningProtein tyrosine phosphatase activityProtein tyrosine phosphataseTyrosine phosphatase activityGlutamate receptor internalizationOptimization of fragmentsTyrosine phosphataseDual specificityReceptor internalizationDevelopment of SelectiveSTEP inhibitorPhosphatase activityAlzheimer's diseaseIonotropic glutamate receptorsSubstrate-based approachNonpeptidic inhibitorsPotential targetAD mouse modelDrug discoveryRat cortical neuronsActivity screeningCortical neuronsGlutamate receptorsMouse modelNeuropsychiatric disorders
2005
Regulation of NMDA receptor trafficking by amyloid-β
Snyder EM, Nong Y, Almeida CG, Paul S, Moran T, Choi EY, Nairn AC, Salter MW, Lombroso PJ, Gouras GK, Greengard P. Regulation of NMDA receptor trafficking by amyloid-β. Nature Neuroscience 2005, 8: 1051-1058. PMID: 16025111, DOI: 10.1038/nn1503.Peer-Reviewed Original ResearchMeSH KeywordsAlpha7 Nicotinic Acetylcholine ReceptorAlzheimer DiseaseAmyloid beta-PeptidesAmyloid beta-Protein PrecursorAnimalsCalcineurinCell MembraneCerebral CortexCREB-Binding ProteinDisease Models, AnimalElectric ConductivityEndocytosisEnzyme ActivationMiceNeuronsN-MethylaspartateNuclear ProteinsPeptide FragmentsProtein TransportProtein Tyrosine PhosphatasesProtein Tyrosine Phosphatases, Non-ReceptorReceptors, NicotinicReceptors, N-Methyl-D-AspartateSignal TransductionSynapsesTrans-ActivatorsConceptsNMDA receptorsCortical neuronsAlzheimer's diseaseBrains of patientsAlzheimer's disease pathologyNMDA receptor traffickingGenetic mouse modelsΓ-secretase inhibitorApplication of amyloidSurface NMDA receptorsGlutamatergic transmissionSynaptic dysfunctionPersistent depressionTyrosine phosphatase STEPNicotinic receptorsMouse modelDisease processSynaptic plasticityDisease pathologyNeuronsReceptorsAmyloidSurface expressionUnderlying mechanismReceptor trafficking