Discovery of a Subnanomolar Helical d-Tridecapeptide Inhibitor of γ-Secretase
- 29 June 2004
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (16) , 3931-3933
- https://doi.org/10.1021/jm049788c
Abstract
γ-Secretase is the second of two proteolytic enzymes responsible for the release of the amyloid β-peptide implicated in the etiology of Alzheimer's disease. Here, we used solid-phase synthesis to generate a new series of helical peptides as γ-secretase inhibitors, one of which, 11, showed an IC50 of 140 pM in a cell-free enzyme assay.Keywords
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