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Description

An eight residue peptidomimetic, tight binding transition-state analog inhibitor of human brain memapsin 2 (Ki = 1.6 nM, recombinant memapsin 2, Ki = 9.58 nM, recombinant pro-memapsin 2). Also inhibits cathepsin D (Ki = 48 nM). This aspartyl protease inhibitor is designed from the template of the beta-secretase site of Swedish beta-amyloid precursor protein (APP) with Asp to Ala replacement, also includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala., A peptidomimetic, highly potent, tight-binding transition-state analog inhibitor of human brain beta-secretase (Ki = 1.6 nM, recombinant memapsin-2, Ki = 9.58 nM, recombinant pro-memapsin 2). Designed from the template of the beta-secretase site of Swedish beta-amyloid precursor protein (APP) with Asp to Ala replacement. Includes a nonhydrolyzable hydroxyethylene isostere between Leu and Ala. Also reported to inhibit cathepsin D at higher levels (Ki = 48 nM).