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Literature summary for 3.4.24.86 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

Inhibitors Comment Organism Structure
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
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

Metals/Ions

Metals/Ions Comment Organism Structure
additional information metalloprotease Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P78536
-
-

Source Tissue

Source Tissue Comment Organism Textmining
EA.hy926 cell
-
Homo sapiens
-
endothelial cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
a disintegrin and metalloprotease 17
-
Homo sapiens
ADAM-17
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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

General Information Comment Organism
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