Discovery and clinical translation of ceperognastat, an O‐GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease
Kielbasa W, Goldsmith P, Donnelly K, Nuthall H, Shcherbinin S, Fleisher A, Hendle J, DuBois S, Lowe S, Zhang F, Woerly E, Dreyfus N, Evans D, Gilmore J, Mancini M, Constantinescu C, Gunn R, Russell D, Collins E, Brys M, Hutton M, Mergott D. Discovery and clinical translation of ceperognastat, an O‐GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease. Alzheimer's & Dementia: Translational Research & Clinical Interventions 2024, 10: e70020. PMID: 39748851, PMCID: PMC11694536, DOI: 10.1002/trc2.70020.Peer-Reviewed Original ResearchReduced tau pathologyO-GlcNAcaseOGA inhibitorsO-GlcNAcO-GlcNAcylationPost-translational modifications of tauTau pathologyAlzheimer's diseaseTau O-GlcNAcylationRemoval of O-GlcNAcModifications of tauO-GlcNAcase inhibitionPost-translational modificationsInhibitor of O-GlcNAcaseO-GlcNAcase inhibitorProgression of ADEnzyme occupancyTauopathy modelPathological tauPhase 1 clinical studyTreatment of Alzheimer's diseaseHuman brainEnzyme activityPatients relative to healthy controlsPotential therapeutic approach
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