Leucyl-cysteinyl aminopeptidase | M1: Aminopeptidase N | IUPHAR/BPS Guide to PHARMACOLOGY

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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

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

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.


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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 23/09/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1570.