Target intelligence / Profile preview

Endothelin-converting enzyme 1 (ECE-1)

Target
ECE-1
Molecular classification
Enzyme, Metalloendopeptidase, Zinc-dependent metalloendopeptidase
01

Overview

Endothelin-converting enzyme 1 (ECE-1) is a zinc-dependent metalloendopeptidase that catalyzes the conversion of inactive big endothelins into their active forms, regulating vascular tone. It also degrades neuropeptides, influencing receptor recycling. ECE-1 exists as four isoforms with differing subcellular localizations. Dysregulation of ECE-1 is implicated in cardiovascular diseases like hypertension and atherosclerosis, making it a therapeutic target for conditions involving abnormal vasoconstriction or endothelial dysfunction.

Other names
ECE1
02

Mechanism of action

Inhibition of ECE-1 prevents the conversion of big endothelins to active endothelins, reducing vasoconstriction and downstream effects.

03

Biological functions

Regulation of blood pressureModulation of inflammatory responsesPromotion of receptor recycling/resensitizationEndothelin biosynthesisNeuropeptide degradation
04

Disease associations

HypertensionAtherosclerosisCardiovascular diseaseVascular injuryInflammation
05

Safety considerations

Potential for affecting multiple vasoactive peptide pathways.Off-target effects due to broad substrate specificity.
06

Interacting drugs

Phosphoramidon

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