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
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 Perspect, 3 (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 Chem, 1 (4): 321-6. [PMID:16789889]

How to cite this page

M13: Neprilysin: Neutral endopeptidase. Last modified on 05/04/2016. Accessed on 19/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1611.