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Literature summary for 3.4.11.7 extracted from

  • David, C.; Bischoff, L.; Meudal, H.; Mothe, A.; De Mota, N.; DaNascimento, S.; Llorens-Cortes, C.; Fournie-Zaluski, M.C.; Roques, B.P.
    Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme (1999), J. Med. Chem., 42, 5197-5211.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH
-
Mus musculus
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH
-
Mus musculus
[[(2R,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2R,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2R,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2R,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentane]-Ile-Asp-OH
-
Mus musculus
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Tyr-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH
-
Mus musculus
[[(2S,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2S,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2S,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH
-
Mus musculus
[[(2S,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH
-
Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus P16406
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Glu-2-naphthylamide + H2O
-
Mus musculus L-Glu + 2-naphthylamine
-
?
additional information the S1' subsite is hydrophobic whereas the S2' subsite recognizes preferentially negatively charged residues derived from aspartic acid Mus musculus ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000032
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.00000356
-
[[(2S,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.0000036
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH pH 7.3, 37°C Mus musculus
0.0000043
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH pH 7.3, 37°C Mus musculus
0.00000536
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH pH 7.3, 37°C Mus musculus
0.0000093
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH pH 7.3, 37°C Mus musculus
0.000012
-
[[(2S,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000013
-
[[(2S,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.0000147
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000015
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000016
-
[[(2R,3S)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.00002
-
[[(2S,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000027
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-Asp-OH pH 7.3, 37°C Mus musculus
0.00004
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH pH 7.3, 37°C Mus musculus
0.00005
-
[[(2R,3S)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000051
-
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentane]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000053
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.0000733
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Tyr-homosulfoalanine-OH pH 7.3, 37°C Mus musculus
0.00008
-
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.0000833
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-3-sulfoalanine-OH pH 7.3, 37°C Mus musculus
0.000145
-
[[(2S,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2 pH 7.3, 37°C Mus musculus
0.00015
-
[[(2RS,3RS)-3-amino2-sulfhydryl-5-sulfamoyl]pentanoyl]-Tyr-Asp-OH pH 7.3, 37°C Mus musculus
0.000267
-
[[(2R,3R)-3-amino-5-carboxylate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.000283
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-D-Asp-OH pH 7.3, 37°C Mus musculus
0.000292
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-D-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.00047
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.00091
-
[[(2R,3R)-3-amino-5-phosphonate-2-sulfhydryl]pentanoyl]-Ile-Asp-OH pH 7.3, 37°C Mus musculus
0.0012
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-OH pH 7.3, 37°C Mus musculus
0.0042
-
[[(2R,3R)-3-amino-2-sulfhydryl-5-sulfonate]pentanoyl]-Ile-NH2 pH 7.3, 37°C Mus musculus