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. 2004 Jul 29;47(16):3931-3.
doi: 10.1021/jm049788c.

Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase

Frédéric Bihel  1 , Chittaranjan Das, Michael J Bowman, Michael S Wolfe
Affiliations

Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase

Frédéric Bihel et al. J Med Chem. .

Abstract

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 IC(50) of 140 pM in a cell-free enzyme assay.

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