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Leucyl-cysteinyl aminopeptidase

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Target not currently curated in GtoImmuPdb

Target id: 1570

Nomenclature: Leucyl-cysteinyl aminopeptidase

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 1025 5q15 LNPEP leucyl and cystinyl aminopeptidase
Mouse 1 1025 17 A3.2 Lnpep leucyl/cystinyl aminopeptidase
Rat 1 1025 1q12 Lnpep leucyl and cystinyl aminopeptidase
Previous and Unofficial Names Click here for help
Otase | Oxytocinase | placental leucine aminopeptidase | cystinyl aminopeptidase | aminopeptidase Vp165 | angiotensin IV receptor | GP160 | insulin-regulated membrane aminopeptidase IRAP | CAP | PLAP | leucyl/cystinyl aminopeptidase
Database Links Click here for help
Specialist databases
MEROPS M01.011 (Hs)
Other databases
Alphafold Q9UIQ6 (Hs), Q8C129 (Mm), P97629 (Rn)
BRENDA 3.4.11.3
ChEMBL Target CHEMBL2693 (Hs), CHEMBL4105715 (Mm), CHEMBL3712 (Rn)
Ensembl Gene ENSG00000113441 (Hs), ENSMUSG00000023845 (Mm), ENSRNOG00000055229 (Rn)
Entrez Gene 4012 (Hs), 240028 (Mm), 171105 (Rn)
Human Protein Atlas ENSG00000113441 (Hs)
KEGG Enzyme 3.4.11.3
KEGG Gene hsa:4012 (Hs), mmu:240028 (Mm), rno:171105 (Rn)
OMIM 151300 (Hs)
Pharos Q9UIQ6 (Hs)
RefSeq Nucleotide NM_005575 (Hs), NM_175920 (Hs), NM_172827 (Mm), NM_001113403 (Rn), NM_133574 (Rn)
RefSeq Protein NP_787116 (Hs), NP_005566 (Hs), NP_766415 (Mm), NP_001106874 (Rn), NP_598258 (Rn)
UniProtKB Q9UIQ6 (Hs), Q8C129 (Mm), P97629 (Rn)
Wikipedia LNPEP (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.11.3

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
inhibitor 19 [PMID: 21476495] Small molecule or natural product Primary target of this compound Hs Inhibition 8.7 pKi 1
⤷ pKi 8.7 (Ki 1.8x10-9 M) [1]
compound 17 [PMID: 23916253] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.2 pIC50 2
⤷ pIC50 5.2 (IC50 6x10-6 M) [2]
Immuno Process Associations
Immuno Process:  Antigen presentation
Immuno Process:  Cellular signalling
General Comments
Leucyl/cystinyl aminopeptidase (LNPEP) is a zinc-dependent aminopeptidase that cleaves vasopressin, oxytocin, lys-bradykinin, met-enkephalin, dynorphin A and other peptide hormones. The protein is found as a secreted form, in intracellular vesicles with the insulin-responsive glucose transporter GLUT4 or as a type II membrane-bound glycoprotein. The protein catalyzes the final step in the conversion of angiotensinogen to angiotensin IV (AT4), and AT4 analogues are being investigated as LNPEP inhibitors.

References

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1. Andersson H, Demaegdt H, Johnsson A, Vauquelin G, Lindeberg G, Hallberg M, Erdelyi M, Karlen A, Hallberg A. (2011) Potent macrocyclic inhibitors of insulin-regulated aminopeptidase (IRAP) by olefin ring-closing metathesis. J Med Chem, 54 (11): 3779-92. [PMID:21476495]

2. 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]

How to cite this page

M1: Aminopeptidase N: Leucyl-cysteinyl aminopeptidase. Last modified on 11/08/2015. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1570.