pH-Dependent Population Shift Regulates BACE1 Activity and Inhibition

BACE1, a major therapeutic target for treatment of Alzheimer’s disease, functions within a narrow pH range. Despite tremendous effort and progress in the development of BACE1 inhibitors, details of the underlying pH-dependent regulatory mechanism remain unclear. Here we elucidate the pH-dependent co...

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Veröffentlicht in:	Journal of the American Chemical Society 2015-08, Vol.137 (30), p.9540-9543
Hauptverfasser:	Ellis, Christopher R, Shen, Jana
Format:	Artikel
Sprache:	eng
Schlagworte:	adverse effects Alzheimer disease Amyloid Precursor Protein Secretases - antagonists & inhibitors Amyloid Precursor Protein Secretases - chemistry Amyloid Precursor Protein Secretases - metabolism Aspartic Acid Endopeptidases - antagonists & inhibitors Aspartic Acid Endopeptidases - chemistry Aspartic Acid Endopeptidases - metabolism Humans Hydrogen-Ion Concentration molecular dynamics Molecular Dynamics Simulation Molecular Structure Oligopeptides - chemistry Oligopeptides - pharmacology Structure-Activity Relationship
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