Endothelin-converting enzyme 1

Target id: 1615

Nomenclature: Endothelin-converting enzyme 1

Abbreviated Name: ECE1

Family: M13: Neprilysin

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Endothelin-converting enzyme 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 770 1p36.1 ECE1 endothelin converting enzyme 1
Mouse - 753 4 D3 Ece1 endothelin converting enzyme 1
Rat - 754 5q36 Ece1 endothelin converting enzyme 1
Previous and Unofficial Names
ECE-1 | ECE
Database Links
Specialist databases
MEROPS M13.002 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.71
Endogenous substrates (Human)
endothelin-1 (EDN1, P05305), endothelin-2 (EDN2, P20800), endothelin-3 (EDN3, P14138)

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 22 [PMID: 19899765] Hs Inhibition 5.9 pKi 2
pKi 5.9 (Ki 1.2x10-6 M) [2]
PD159790 Hs Inhibition 5.6 pKi 1
pKi 5.6 (Ki 2.3x10-6 M) [1]
SM19712 Rn Inhibition 7.4 pIC50 4
pIC50 7.4 (IC50 4.2x10-8 M) [4]
KC-12615 Hs Inhibition 5.8 pIC50 3
pIC50 5.8 (IC50 1.5x10-6 M) [3]
daglutril Hs Inhibition - -
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Hirschsprung disease, cardiac defects, and autonomic dysfunction
OMIM: 613870
Disease:  Hypertension, essential
Disease Ontology: DOID:10825
OMIM: 145500

References

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1. Ahn K, et al. (1996) Quinazolines as inhibitors of endothelin converting enzyme. Patent number: WO1996019474. Assignee: Warner Lambert. Priority date: 22/12/1994. Publication date: 22/06/1996.

2. Jullien N, Makritis A, Georgiadis D, Beau F, Yiotakis A, Dive V. (2010) Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. J. Med. Chem.53 (1): 208-20. [PMID:19899765]

3. Seed A, Kuc RE, Maguire JJ, Hillier C, Johnston F, Essers H, de Voogd HJ, McMurray J, Davenport AP. (2012) The dual endothelin converting enzyme/neutral endopeptidase inhibitor SLV-306 (daglutril), inhibits systemic conversion of big endothelin-1 in humans. Life Sci.91 (13-14): 743-8. [PMID:22480515]

4. Umekawa K, Hasegawa H, Tsutsumi Y, Sato K, Matsumura Y, Ohashi N. (2000) Pharmacological characterization of a novel sulfonylureid-pyrazole derivative, SM-19712, a potent nonpeptidic inhibitor of endothelin converting enzyme. Jpn. J. Pharmacol.84 (1): 7-15. [PMID:11043447]

How to cite this page

M13: Neprilysin: Endothelin-converting enzyme 1. Last modified on 21/07/2015. Accessed on 12/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1615.