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Literature summary for 3.4.24.B14 extracted from

  • Voisin, S.; Rognan, D.; Gros, C.; Ouimet, T.
    A three-dimensional model of the neprilysin 2 active site based on the X-ray structure of neprilysin. Identification of residues involved in substrate hydrolysis and inhibitor binding of neprilysin 2 (2004), J. Biol. Chem., 279, 46172-46181.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
angiotensin
-
Rattus norvegicus
bradykinin
-
Rattus norvegicus
cholecystokinin(1-6)
-
Rattus norvegicus
cholecystokinin-8
-
Rattus norvegicus
Leu-Met
-
Rattus norvegicus
Leu-Met-NH2
-
Rattus norvegicus
Leu5-enkephalin
-
Rattus norvegicus
Leu5-enkephalin-NH2
-
Rattus norvegicus
Substance P
-
Rattus norvegicus
Val-Phe
-
Rattus norvegicus
Val-Phe-NH2
-
Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.04
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme L739G Rattus norvegicus
0.044
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme L739G/S133G Rattus norvegicus
0.045
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme R131M Rattus norvegicus
0.062
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2. wild-type enzyme Rattus norvegicus
0.185
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme S133G Rattus norvegicus
1
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme N567G Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
angiotensin + H2O cleavage sites: DRVY-/-IHP-/-FHL Rattus norvegicus ?
-
?
bradykinin + H2O cleavage sites: RPPGFSP-/-FR Rattus norvegicus ?
-
?
cholecystokinin(1-6) + H2O cleavage site: DYMG-/-WM Rattus norvegicus ?
-
?
cholecystokinin-8 + H2O cleavage site: DYMG-/-WMDF-NH2 Rattus norvegicus ?
-
?
Leu5-enkephalin + H2O cleavage site: YGG-/-FL Rattus norvegicus ?
-
?
Leu5-enkephalin-NH2 + H2O cleavage site: YGG-/-FL-NH2 Rattus norvegicus ?
-
?
Substance P + H2O cleavage sites: RPKPQQ-/-FFG-/-LM-NH2 Rattus norvegicus ?
-
?
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide + H2O
-
Rattus norvegicus succinyl-Ala-Ala + Phe-4-methylcoumarin 7-amide
-
?

Synonyms

Synonyms Comment Organism
NEP2
-
Rattus norvegicus
neprilysin 2
-
Rattus norvegicus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.52
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
1.97
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme S133G Rattus norvegicus
5.23
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme N567G Rattus norvegicus
14.03
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
17.3
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme R131M Rattus norvegicus
19
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme L739G/S133G Rattus norvegicus
30.7
-
succinyl-Ala-Ala-Phe-4-methylcoumarin 7-amide 37°C, pH 7.2, mutant enzyme L739G Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
Leu5-enkephalin 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.003
-
bradykinin 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.008
-
angiotensin 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.01
-
cholecystokinin-8 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.011
-
Substance P 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.02
-
Leu-Met 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.02
-
Leu5-enkephalin-NH2 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.021
-
Val-Phe 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.05
-
cholecystokinin(1-6) 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.13
-
Val-Phe-NH2 37°C, pH 7.2, wild-type enzyme Rattus norvegicus
0.175
-
Leu-Met-NH2 37°C, pH 7.2, wild-type enzyme Rattus norvegicus