L-685,458, an Aspartyl Protease Transition State Mimic, Is a Potent Inhibitor of Amyloid β-Protein Precursor γ-Secretase Activity

作者: Mark S. Shearman , Dirk Beher , Earl E. Clarke , Huw D. Lewis , Tim Harrison

DOI: 10.1021/BI0005456

关键词: P3 peptideProtein precursorPeptide sequenceBiochemistryChemistryPresenilinGene mutationMolecular mimicryStructure–activity relationshipAmyloid precursor protein secretase

摘要: … inhibition of Aβ(42) and Aβ(40) peptides. This compound contains an hydroxyethylene dipeptide … The preferred stereochemistry of the hydroxyethylene dipeptide isostere was found to …

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