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Literature summary for 3.4.23.46 extracted from

  • Ghosh, A.K.; Kumaragurubaran, N.; Hong, L.; Kulkarni, S.; Xu, X.; Miller, H.B.; Reddy, D.S.; Weerasena, V.; Turner, R.; Chang, W.; Koelsch, G.; Tang, J.
    Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation (2008), Bioorg. Med. Chem. Lett., 18, 1031-1036.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
 Homo sapiens
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide up to 65% reduction of plasma amyloid beta in transgenic mice Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg-Glu(EDANS)-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys(Dabcyl)-Arg + H2O
-
 Homo sapiens ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000018
-
 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide pH 4.5, 37°C Homo sapiens