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Literature summary for 3.4.24.11 extracted from

  • McKinnie, S.M.; Fischer, C.; Tran, K.M.; Wang, W.; Mosquera, F.; Oudit, G.Y.; Vederas, J.C.
    The metalloprotease neprilysin degrades and inactivates apelin peptides (2016), ChemBioChem, 17, 1495-1498 .
    View publication on PubMed

Application

Application Comment Organism
medicine NEP is a target for Entresto used in treatment of heart failure Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
EDTA complete inhibition Homo sapiens
additional information structure-activity relationship studies. No or poor inhibition by 4-(2-aminoethyl)benzylsulfonyl fluoride (AEBSF), and Nalpha-tosyl-l-lysyl chloromethylketone (TLCK), and iodoacetamide Homo sapiens
PMSF weak inhibition Homo sapiens
thiorphan complete inhibition Homo sapiens
tris(2-carboxyethyl)phosphine TCEP, strong inhibition Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P08473
-
-

Purification (Commentary)

Purification (Comment) Organism
native enzyme from human blood plasma by ammonium sulfate fractionation, and gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-
heart
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 KFRRQRPRLSHKGPMPF + 2 H2O
-
Homo sapiens KFRRQRPR + LSHKGPMPF + KFRRQRPRL + SHKGPMPF
-
ir
2 LVQPRGSRNGPGPWQGGRRKFRRQRPRLSHKGPMPF + 2 H2O
-
Homo sapiens LVQPRGSRNGPGPWQGGRRKFRRQRPRL + SHKGPMPF + LVQPRGSRNGPGPWQGGRRKFRRQRPR + LSHKGPMPF
-
ir
2 pGlu-RPRLSHKGPMPF + 2 H2O
-
Homo sapiens pGlu-RPRL + pGlu-RPR + SHKGPMPF + LSHKGPMPF
-
ir
Abz-QRPRLSH-(3-nitro)Tyr + H2O
-
Homo sapiens Abz-QRPRL + Ser-His-(3-nitro)Tyr
-
ir
additional information in vitro NEP proteolysis generates fragments that lack the ability to bind to the apelin receptor, NEP fully inactivates apelin Homo sapiens ?
-
-
additional information in vitro NEP proteolysis generates fragments that lack the ability to bind to the apelin receptor, NEP fully inactivates apelin Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
NEP
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5 6 isoelectric focusing Homo sapiens
6.5
-
enzyme assay Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
6.5 9 activity range, no activity at pH 5.0 Homo sapiens

General Information

General Information Comment Organism
physiological function the metalloprotease neprilysin degrades and inactivates apelin peptides. The apelinergic system is a mammalian peptide hormone network with key physiological roles. Apelin isoforms and analogues are believed to be promising therapeutics for cardiovascular disease. Involvement of NEP in the apelinergic system. In vitro NEP proteolysis generates fragments that lack the ability to bind to the apelin receptor, NEP protease fully inactivates apelin Homo sapiens