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Endoplasmic reticulum aminopeptidase 1

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Target not currently curated in GtoImmuPdb

Target id: 1566

Nomenclature: Endoplasmic reticulum aminopeptidase 1

Family: M1: Aminopeptidase N

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 941 5q15 ERAP1 endoplasmic reticulum aminopeptidase 1
Mouse 1 930 13 C1 Erap1 endoplasmic reticulum aminopeptidase 1
Rat 1 930 2q11 Erap1 endoplasmic reticulum aminopeptidase 1
Previous and Unofficial Names Click here for help
Adipocyte-derived leucine aminopeptidase | puromycin-insensitive leucyl-specific aminopeptidase | aminopeptidase regulator of TNFR1 shedding | aminopeptidase PILS | Arts1 | ER-aminopeptidase 1 | leucyl-specific aminopeptidase PILS | ERAAP | A-LAP | ERAAP1 | PILS-AP
Database Links Click here for help
Specialist databases
MEROPS M01.018 (Hs)
Other databases
Alphafold Q9NZ08 (Hs), Q9EQH2 (Mm), Q9JJ22 (Rn)
BRENDA 3.4.11.-
ChEMBL Target CHEMBL5939 (Hs), CHEMBL3414412 (Mm)
Ensembl Gene ENSG00000164307 (Hs), ENSMUSG00000021583 (Mm), ENSRNOG00000009997 (Rn)
Entrez Gene 51752 (Hs), 80898 (Mm), 80897 (Rn)
Human Protein Atlas ENSG00000164307 (Hs)
KEGG Enzyme 3.4.11.-
KEGG Gene hsa:51752 (Hs), mmu:80898 (Mm), rno:80897 (Rn)
OMIM 606832 (Hs)
Pharos Q9NZ08 (Hs)
RefSeq Nucleotide NM_001198541 (Hs), NM_001040458 (Hs), NM_016442 (Hs), NM_030711 (Mm)
RefSeq Protein NP_057526 (Hs), NP_001035548 (Hs), NP_001185470 (Hs), NP_109636 (Mm)
UniProtKB Q9NZ08 (Hs), Q9EQH2 (Mm), Q9JJ22 (Rn)
Wikipedia ERAP1 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.11.-

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 2g [PMID: 27390066] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.3 pKi 2
⤷ pKi 6.3 (Ki 5.3x10-7 M) [2]
compound 3v [PMID: 27390066] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition <3.6 pKi 2
⤷ pKi <3.6 (Ki >2.5x10-4 M) [2]
compound 17 [PMID: 23916253] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.6 pIC50 1
⤷ pIC50 5.6 (IC50 2.6x10-6 M) [1]
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)

References

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1. Papakyriakou A, Zervoudi E, Theodorakis EA, Saveanu L, Stratikos E, Vourloumis D. (2013) Novel selective inhibitors of aminopeptidases that generate antigenic peptides. Bioorg Med Chem Lett, 23 (17): 4832-6. [PMID:23916253]

2. Węglarz-Tomczak E, Vassiliou S, Mucha A. (2016) Discovery of potent and selective inhibitors of human aminopeptidases ERAP1 and ERAP2 by screening libraries of phosphorus-containing amino acid and dipeptide analogues. Bioorg Med Chem Lett, 26 (16): 4122-6. [PMID:27390066]

How to cite this page

M1: Aminopeptidase N: Endoplasmic reticulum aminopeptidase 1. Last modified on 20/10/2017. Accessed on 30/04/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1566.