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Literature summary extracted from

  • Kuruppu, S.; Rajapakse, N.W.; Minond, D.; Smith, A.I.
    Production of soluble neprilysin by endothelial cells (2014), Biochem. Biophys. Res. Commun., 446, 423-427.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.11 additional information no inhibition by 4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione and 4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione Homo sapiens
3.4.24.11 thiorphan
-
Homo sapiens
3.4.24.86 4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione synthesis of the specific inhibitor, overview Homo sapiens
3.4.24.86 4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione synthesis of the specific inhibitor, overview Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.24.11 extracellular
-
Homo sapiens
-
-
3.4.24.11 additional information the enzyme is released from endothelial cells via exosomes, the process is dependent on ADAM-17 protease Homo sapiens
-
-
3.4.24.11 soluble
-
Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.24.86 additional information metalloprotease Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.24.11 bradykinin + H2O Homo sapiens
-
?
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.11 Homo sapiens P08473
-
-
3.4.24.86 Homo sapiens P78536
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.24.11 EA.hy926 cell
-
Homo sapiens
-
3.4.24.11 endothelial cell
-
Homo sapiens
-
3.4.24.86 EA.hy926 cell
-
Homo sapiens
-
3.4.24.86 endothelial cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.11 (7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys-(2,4-dinitrophenyl) + H2O bradykinin-based quenched fluorescent substrate assay Homo sapiens (7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala + Phe-Lys-(2,4-dinitrophenyl)
-
?
3.4.24.11 bradykinin + H2O
-
Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.24.11 CALLA
-
Homo sapiens
3.4.24.11 CD10
-
Homo sapiens
3.4.24.11 common acute lymphoblastic leukemia antigen
-
Homo sapiens
3.4.24.11 endopeptidase-24.11
-
Homo sapiens
3.4.24.11 enkephalinase
-
Homo sapiens
3.4.24.11 NEP
-
Homo sapiens
3.4.24.86 a disintegrin and metalloprotease 17
-
Homo sapiens
3.4.24.86 ADAM-17
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.24.11 37
-
assay at Homo sapiens
3.4.24.86 22
-
assay at room temperature Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.24.11 6.3
-
assay at Homo sapiens
3.4.24.86 7.5
-
assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.86 0.00432
-
pH 7.5, 22°C Homo sapiens 4-(cyclopentylmethyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione
3.4.24.86 0.00536
-
pH 7.5, 22°C Homo sapiens 4-(2-butylbenzyl)-5-(4-hydroxybenzyl)-1-[1-(2-[[6-(4-hydroxybenzyl)-2,3-dioxopiperazin-1-yl]methyl]pyrrolidin-1-yl)-3-(naphthalen-2-yl)propan-2-yl]piperazine-2,3-dione

General Information

EC Number General Information Comment Organism
3.4.24.11 malfunction treatment of cells with TPI2155-14 and TPI2155-17, specific inhibitors for ADAM-17 protease, EC 3.4.24.86, results in a significant decrease in neprilysin activity in media, implicating a possible role for ADAM-17 in neprilysin release Homo sapiens
3.4.24.11 metabolism the non-membrane bound form of neprilysin with catalytic activity has the potential to cleave substrates throughout the blood circulation with systemic effects. A likely role of exosomes and protease ADAM-17 in release of the enzyme, overview Homo sapiens
3.4.24.86 physiological function treatment of cells with TPI2155-14 and TPI2155-17, specific inhibitors for ADAM-17 protease, results in a significant decrease in non-membrane bound form of neprilysin, EC 3.4.24.11, activity in media, implicating a possible role for ADAM-17 in neprilysin release Homo sapiens