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Literature summary for 3.4.24.56 extracted from

  • Song, E.S.; Daily, A.; Fried, M.G.; Juliano, M.A.; Juliano, L.; Hersh, L.B.
    Mutation of active site residues of insulin-degrading enzyme alters allosteric interactions (2005), J. Biol. Chem., 280, 17701-17706.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
E111A change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is dampened. Mutant recognizes additional cleavage sites in substrate beta-endorphin Rattus norvegicus
E111F change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is dampened. Mutant recognizes additional cleavage sites in substrate beta-endorphin Rattus norvegicus
E111L change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is dampened. Mutant recognizes additional cleavage sites in substrate beta-endorphin Rattus norvegicus
E111V change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is dampened. Mutant recognizes additional cleavage sites in substrate beta-endorphin Rattus norvegicus
H112D change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is changed to inhibition. Affinity to Zn2+ is lower than in wild-type Rattus norvegicus
H112Q change in the substrate response from sigmoidal to hyperbolic. Activating effect of ATP or triphosphate with substrate 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) on wild-type is changed to inhibition. Affinity to Zn2+ is lower than in wild-type Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
EDTA 0.1 mM, wild-type, 91% residual activity, mutants H112D, H112Q, less than 2.5% residual activity Rattus norvegicus
o-phenanthroline 0.1 mM, wild-type, 73% residual activity, mutants H112D, H112Q, less than 2.5% residual activity Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111L, pH 7.3 Rattus norvegicus
0.0156
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111V, pH 7.3 Rattus norvegicus
0.0274
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111F, pH 7.3 Rattus norvegicus
0.0287
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) wild-type, K0.5-value, pH 7.3 Rattus norvegicus
0.083
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant H112D, pH 7.3 Rattus norvegicus
0.158
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant H112Q, pH 7.3 Rattus norvegicus
0.204
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111A, pH 7.3 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) + H2O
-
Rattus norvegicus ?
-
?
amyloid beta-protein + H2O
-
Rattus norvegicus ?
-
?
beta-endorphin + H2O
-
Rattus norvegicus ?
-
?
insulin + H2O
-
Rattus norvegicus ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2 3.7 2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant H112D, pH 7.3 Rattus norvegicus
2.4
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111V, pH 7.3 Rattus norvegicus
6.5
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111L, pH 7.3 Rattus norvegicus
11.4
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111F, pH 7.3 Rattus norvegicus
17.5
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant E111A, pH 7.3 Rattus norvegicus
1953
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) mutant H112Q, pH 7.3 Rattus norvegicus
162600
-
2-aminobenzoyl-GGFLRKHGQ-(N-(2,4-dinitrophenyl)ethylenediamine) wild-type, pH 7.3 Rattus norvegicus