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
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 18/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1615.