Discovery of a Subnanomolar Helical <scp>d</scp>-Tridecapeptide Inhibitor of γ-Secretase
作者:Frédéric Bihel、Chittaranjan Das、Michael J. Bowman、Michael S. Wolfe
DOI:10.1021/jm049788c
日期:2004.7.1
gamma-Secretase is the second of two proteolytic enzymes responsible for the release of the amyloid beta-peptide implicated in the etiology of Alzheimer's disease. Here, we used solid-phase synthesis to generate a new series of helical peptides as gamma-secretase inhibitors, one of which, 11, showed an IC50 of 140 muM in a cell-free enzyme assay.