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Bioorg Med Chem Lett. 2009 Jan 1;19(1):17-20. doi: 10.1016/j.bmcl.2008.11.027. Epub 2008 Nov 13.

Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co, West Point, PA 19486, USA.

Abstract

A small molecule inhibitor of beta-secretase with a unique binding mode has been developed. Crystallographic determination of the enzyme-inhibitor complex shows the catalytic aspartate residues in the active site are not engaged in inhibitor binding. This unprecedented binding mode in the field of aspartyl protease inhibition is described.

PMID:
19036583
DOI:
10.1016/j.bmcl.2008.11.027
[Indexed for MEDLINE]

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