Access through your institution Buy or subscribe The β-secretase-mediated generation of amyloid-β peptide (Aβ) is involved in the pathogenesis of Alzheimer's disease. This paper

describes the characterization of the first orally available non-peptidic β-secretase inhibitor, LY2811376. The β-secretase 1 (BACE1) inhibitor, which was identified by fragment-based

screening, lowered Aβ levels in a mouse model of Alzheimer's disease as well as in normal dogs. In healthy volunteers LY2811376 was safe and well tolerated and produced long-lasting

reductions in Aβ levels. Although the authors note that non-target-related toxicology prevented the compound from progressing to clinical development, this study shows that BACE1 is a

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PAPER * May, P. C. et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. _J. Neurosci._ 31, 16507–16516 (2011)Article Article 

CAS  Google Scholar  Download references Authors * Charlotte Harrison View author publications You can also search for this author inPubMed Google Scholar RIGHTS AND PERMISSIONS Reprints and

permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Harrison, C. Inhibiting β-secretase in humans. _Nat Rev Drug Discov_ 11, 21 (2012). https://doi.org/10.1038/nrd3645 Download citation *

Published: 03 January 2012 * Issue Date: January 2012 * DOI: https://doi.org/10.1038/nrd3645 SHARE THIS ARTICLE Anyone you share the following link with will be able to read this content:

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