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Literature summary for 3.4.11.3 extracted from

  • Ye, S.; Chai, S.Y.; Lew, R.A.; Albiston, A.L.
    Insulin-regulated aminopeptidase: analysis of peptide substrate and inhibitor binding to the catalytic domain (2007), Biol. Chem., 388, 399-403.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in HEK-293T cell Homo sapiens

Protein Variants

Protein Variants Comment Organism
A429G no activity with L-Arg-vasopressin, no activity with L-Leu-enkephalin Homo sapiens
G428D 80% of wild-type activity with L-Arg-vasopressin, no activity with L-Leu-enkephalin Homo sapiens
G428E 50% of wild-type activity with L-Arg-vasopressin, no activity with L-Leu-enkephalin Homo sapiens
G428Q more than wild-type activity with L-Arg-vasopressin, less than 10% of wild-type activity with L-Leu-enkephalin Homo sapiens
N432A no activity with L-Arg-vasopressin, or L-Leu-enkephalin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
L-Arg-vasopressin Ki-value for wild-type, mutants G428E, G428D, G428Q above 0.03 mM Homo sapiens
L-Leu-enkephalin
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.045
-
L-Leu-2-naphthylamide mutant N432A, 37°C Homo sapiens
0.0632
-
L-Leu-2-naphthylamide wild-type, 37°C Homo sapiens
0.087
-
L-Leu-2-naphthylamide mutant G428Q, 37°C Homo sapiens
0.119
-
L-Leu-2-naphthylamide mutant G428E, 37°C Homo sapiens
0.124
-
L-Leu-2-naphthylamide mutant G428D, 37°C Homo sapiens
0.132
-
L-Leu-2-naphthylamide mutant A429G, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Arg-vasopressin + H2O
-
Homo sapiens L-Arg + vasopressin
-
?
L-Leu-2-naphthylamide + H2O
-
Homo sapiens L-Leu + 2-naphthylamine
-
?
L-Leu-enkephalin + H2O
-
Homo sapiens L-Leu + enkephalin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.003
-
L-Arg-vasopressin mutant A429G, 37°C Homo sapiens
0.016
-
L-Arg-vasopressin mutant N432A, 37°C Homo sapiens
0.335
-
L-Leu-enkephalin mutant N432A, 37°C Homo sapiens
0.417
-
L-Leu-enkephalin mutant A429G, 37°C Homo sapiens
0.711
-
L-Leu-enkephalin wild-type, 37°C Homo sapiens
2.06
-
L-Leu-enkephalin mutant G428Q, 37°C Homo sapiens
2.44
-
L-Leu-enkephalin mutant G428D, 37°C Homo sapiens
3.17
-
L-Leu-enkephalin mutant G428E, 37°C Homo sapiens