Leucyl-cysteinyl aminopeptidase

Target id: 1570

Nomenclature: Leucyl-cysteinyl aminopeptidase

Family: M1: Aminopeptidase N

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Leucyl-cysteinyl aminopeptidase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1025 5q15 LNPEP leucyl and cystinyl aminopeptidase
Mouse - 1025 17 A3.2 Lnpep leucyl/cystinyl aminopeptidase
Rat - 1025 1q12 Lnpep leucyl and cystinyl aminopeptidase
Previous and Unofficial Names
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
Specialist databases
MEROPS M01.011 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.11.3

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
inhibitor 19 [PMID: 21476495] Hs Inhibition 8.7 pKi 1
pKi 8.7 (Ki 1.8x10-9 M) [1]
compound 17 [PMID: 23916253] Hs Inhibition 5.2 pIC50 2
pIC50 5.2 (IC50 6x10-6 M) [2]
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 20/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1570.