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J Med Chem. 2004 Dec 16;47(26):6447-50.

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA. shawn_stachel@merck.com

Abstract

We describe the development of cell-permeable beta-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50 < 100 nM), these inhibitors display impressive selectivity against other biologically relevant aspartyl proteases.

PMID:
15588077
DOI:
10.1021/jm049379g
[Indexed for MEDLINE]
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