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Literature summary for 3.4.24.71 extracted from

  • Raoch, V.; Martinez-Miguel, P.; Arribas-Gomez, I.; Rodriguez-Puyol, M.; Rodriguez-Puyol, D.; Lopez-Ongil, S.
    The peptidase inhibitor CGS-26303 increases endothelin converting enzyme-1 expression in endothelial cells through accumulation of big endothelin-1 (2007), Br. J. Pharmacol., 152, 313-322.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
additional information the peptidase inhibitor CGS-26303, bigendothelin-1, and phosphoramidon, though not thiorphan, a neutral endopeptidase inhibitor, increase endothelin converting enzyme-1 expression in endothelial cells through accumulation of big endothelin-1, CGS-26303 and big endothelin increase ECE-1 promoter activity, the stimulation is abolished by cycloheximide, overview Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
CGS-26303 specific, complete inhibition at 0.025 mM Bos taurus
CGS-35066 a selective ECE-1 inhibitor, mimicks the effects of CGS-26303 Bos taurus
additional information neither exogenously added ET-1 nor the blockade of the receptors with bosentan modifies ECE-1 protein, overview Bos taurus
phosphoramidon complete inhibition at 0.1 mM Bos taurus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Bos taurus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
big endothelin-1 + H2O Bos taurus activation endothelin-1 + ?
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
aorta
-
Bos taurus
-
endothelial cell
-
Bos taurus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
big endothelin-1 + H2O activation Bos taurus endothelin-1 + ?
-
?

Synonyms

Synonyms Comment Organism
ECE-1
-
Bos taurus
endothelin-converting enzyme-1
-
Bos taurus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Bos taurus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Bos taurus