Neutral endopeptidase

Target id: 1611

Nomenclature: Neutral endopeptidase

Family: M13: Neprilysin

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Neutral endopeptidase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 750 3q25.2 MME membrane metalloendopeptidase
Mouse - 750 3 E1 Mme membrane metallo endopeptidase
Rat - 750 2q31 Mme membrane metallo-endopeptidase
Previous and Unofficial Names
Enkephalinase | NEP | neprilysin | atriopeptidase | SFE | skin fibroblast elastase | CALLA | CD10 | membrane metallo-endopeptidase
Database Links
Specialist databases
MEROPS M13.001 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.11
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
enkephalins Hs - -

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
compound 1b [PMID: 18078750] Hs Inhibition 8.9 pKi 3
pKi 8.9 (Ki 1.3x10-9 M) [3]
compound 1a [PMID: 25692029] Hs Inhibition 8.9 pKi 1-2
pKi 8.9 (Ki 1.4x10-9 M) [1-2]
fasidotrilat Hs Inhibition 8.3 pKi 7
pKi 8.3 (Ki 5.6x10-9 M) [7]
KC-12615 Hs Inhibition 8.4 pIC50 4
pIC50 8.4 (IC50 4.2x10-9 M) [4]
sacubitrilat Hs Inhibition 8.1 pIC50 6
pIC50 8.1 (IC50 7.3x10-9 M) [6]
candoxatrilat Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.8x10-8 M) [5]
thiorphan Hs Inhibition - -
candoxatril Hs Inhibition - -
fasidotril Hs Inhibition - -
daglutril Hs Inhibition - -
Clinically-Relevant Mutations and Pathophysiology
Disease:  Membranous nephropathy, susceptibility to; MBNP
OMIM: 614692

References

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1. Bonnard E, Poras H, Nadal X, Maldonado R, Fournié-Zaluski MC, Roques BP. (2015) Long-lasting oral analgesic effects of N-protected aminophosphinic dual ENKephalinase inhibitors (DENKIs) in peripherally controlled pain. Pharmacol Res Perspect3 (2): e00116. [PMID:25692029]

2. Chen H, Noble F, Roques BP, Fournié-Zaluski MC. (2001) Long lasting antinociceptive properties of enkephalin degrading enzyme (NEP and APN) inhibitor prodrugs. J. Med. Chem.44 (21): 3523-30. [PMID:11585456]

3. Deaton DN, Gao EN, Graham KP, Gross JW, Miller AB, Strelow JM. (2008) Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite. Bioorg. Med. Chem. Lett.18 (2): 732-7. [PMID:18078750]

4. Figueroa F, Davicino R, Micalizzi B, Oliveros L, Forneris M. (2012) Macrophage secretions modulate the steroidogenesis of polycystic ovary in rats: effect of testosterone on macrophage pro-inflammatory cytokines. Life Sci.90 (19-20): 733-9. [PMID:22480516]

5. Leung D, Abbenante G, Fairlie DP. (2000) Protease inhibitors: current status and future prospects. J. Med. Chem.43 (3): 305-41. [PMID:10669559]

6. Swedberg K. Inhibition of the renin - angiotensin system – present and future challenges. Accessed on 02/11/2014. Modified on 02/11/2014. Heart Failure Update 2014, http://www.hfupdate.ca/pdfs/Inhibition%20of%20th%20eRenin-Angiotensin%20System_Present%20and%20Future%20Challenges_Dr.%20Swedberg.pdf

7. Tsantili-Kakoulidou A, Nicolaou I, Vrakas D, Demopoulos VJ. (2005) Modelling of aldose reductase inhibitory activity of pyrrol-1-yl-acetic acid derivatives by means of multivariate statistics. Med Chem1 (4): 321-6. [PMID:16789889]

How to cite this page

M13: Neprilysin: Neutral endopeptidase. Last modified on 05/04/2016. Accessed on 20/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1611.