2017
X‑ray Characterization and Structure-Based Optimization of Striatal-Enriched Protein Tyrosine Phosphatase Inhibitors
Witten MR, Wissler L, Snow M, Geschwindner S, Read JA, Brandon NJ, Nairn AC, Lombroso PJ, Käck H, Ellman JA. X‑ray Characterization and Structure-Based Optimization of Striatal-Enriched Protein Tyrosine Phosphatase Inhibitors. Journal Of Medicinal Chemistry 2017, 60: 9299-9319. PMID: 29116812, PMCID: PMC5758861, DOI: 10.1021/acs.jmedchem.7b01292.Peer-Reviewed Original ResearchConceptsStriatal-enriched protein tyrosine phosphataseProtein tyrosine phosphatase inhibitorProtein tyrosine phosphataseTyrosine phosphatase inhibitorFirst X-ray crystal structureTyrosine phosphatasePhosphatase inhibitorSTEP inhibitorPhosphorylation levelsInhibitor structureSubstrate-based approachNumerous neuropsychiatric disordersX-ray crystal structureDrug discoverySTEP substratesStructural informationPhosphataseInhibitorsMouse modelKnockdownSurprising findingCrystal structureNeuropsychiatric disordersExcessive activityAlzheimer's disease
2007
S-Nitrosylation and uncompetitive/fast off-rate (UFO) drug therapy in neurodegenerative disorders of protein misfolding
Nakamura T, Lipton S. S-Nitrosylation and uncompetitive/fast off-rate (UFO) drug therapy in neurodegenerative disorders of protein misfolding. Cell Death & Differentiation 2007, 14: 1305-1314. PMID: 17431424, DOI: 10.1038/sj.cdd.4402138.Peer-Reviewed Original ResearchConceptsS-nitrosylationProtein functionProtein misfoldingCell deathNeuronal cell deathProper protein foldingProtein disulfide isomeraseCysteine thiol groupsHeat shock proteinsExcessive NMDA receptor activityGlucose-regulated protein 78Neurodegenerative disordersProtein foldingExcitotoxic damageFree radical nitric oxideConformational changesMisfoldingForm of neurotoxicityRadical nitric oxideN-methyl-D-aspartate receptorsNitric oxideExcessive activityProteinProtein 78Chronic neurodegenerative disorders
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