2p83

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File:2p83.jpg


2p83, resolution 2.500Å

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Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1

OverviewOverview

The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.

About this StructureAbout this Structure

2P83 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Memapsin 2, with EC number 3.4.23.46 Full crystallographic information is available from OCA.

ReferenceReference

Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1., Kortum SW, Benson TE, Bienkowski MJ, Emmons TL, Prince DB, Paddock DJ, Tomasselli AG, Moon JB, LaBorde A, TenBrink RE, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3378-83. Epub 2007 Apr 3. PMID:17434734

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