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Literature summary extracted from

  • Hanson, A.L.; Morton, C.J.; Parker, M.W.; Bessette, D.; Kenna, T.J.
    The genetics, structure and function of the M1 aminopeptidase oxytocinase subfamily and their therapeutic potential in immune-mediated disease (2019), Hum. Immunol., 80, 281-289 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.11.3 gene LNPEP, located on chromosome 5q15 Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.11.3 several crystal structures of enzyme IRAP in apo and ligand boudn states are available, PDB IDs 4P8Q, 4PJ6, 4Z7I, 5C97, and 5MJ6 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.11.3 DG002A
-
 Homo sapiens
3.4.11.3 DG002B
-
 Homo sapiens
3.4.11.3 DG013A
-
 Homo sapiens
3.4.11.3 DG013B
-
 Homo sapiens
3.4.11.3 DG023
-
 Homo sapiens
3.4.11.3 DG026
-
 Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.11.3 Zn2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.11.3 oxytocin + H2O Homo sapiens
-
 ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.11.3 Homo sapiens Q9UIQ6
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.11.3 L-arginine-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens L-arginine + 7-amino-4-methylcoumarin
-
 ?
3.4.11.3 L-leucine-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens L-leucine + 7-amino-4-methylcoumarin
-
 ?
3.4.11.3 oxytocin + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.11.3 LNPEP
-
 Homo sapiens
3.4.11.3 M1 aminopeptidase
-
 Homo sapiens
3.4.11.3 oxytocinase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.11.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens DG023
3.4.11.3 0.00003
-
 pH and temperature not specified in the publication Homo sapiens DG013A
3.4.11.3 0.000032
-
 pH and temperature not specified in the publication Homo sapiens DG026
3.4.11.3 0.000218
-
 pH and temperature not specified in the publication Homo sapiens DG002A
3.4.11.3 0.000344
-
 pH and temperature not specified in the publication Homo sapiens DG002B
3.4.11.3 0.0022
-
 pH and temperature not specified in the publication Homo sapiens DG013B

General Information

EC Number General Information Comment Organism
3.4.11.3 evolution IRAP is a member of the oxytocinase subfamily of M1 aminopeptidases characterised by the presence of two key sequence motifs, the HEXXH zinc-binding and GXMEN substrate recognition sequences Homo sapiens
3.4.11.3 additional information analysis of the structure of IRAP in an intermediate semi-close conformation, overview. Significant rearrangements of the GAMEN motif in IRAP are observed upon ligand binding, which couples to the transition between the original partially open and a new, fully closed conformation of the protein. Molecular dynamics simulations of IRAP focusing on local adaptation to the binding of a pseudopeptidic ligand Homo sapiens