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Literature summary for 3.4.21.108 extracted from

  • Singh, N.; DSouza, A.; Cholleti, A.; Sastry, G.M.; Bose, K.
    Dual regulatory switch confers tighter control on HtrA2 proteolytic activity (2014), FEBS J., 281, 2456-2470.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
inhibitor of apoptosis protein in presence of inhibitor of apoptosis protein, catalytic efficiency increases up to 3fold. In presence of its BIR2 and/or BIR3 domains, catalytic efficiency increases up to 2fold. Interaction allosterically modulates HtrA2 activity, the activation occurs through a series of coordinated structural reorganizations at distal regulatory loops, leading to a population shift towards the relaxed conformer Homo sapiens
PDZ domain G230A mutation in recognition sequence of the PDZ domain, shows a significant decrease in the catalytic efficiency Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information deletion mutant of the PDZ domain shows a catalytic efficiency 5.5fold less than intact trimeric HtrA2 and the apparent Km and co-operativity are also reduced. Deletion of the PDZ domain possibly affects the initial substrate binding process, allosteric modulation and cleavage, thereby leading to a decrease in co-operativity and catalytic efficiency Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0014
-
beta-casein PDZ domain deletion mutant, K0.5 value, Hill constant 1.7, 37°C, pH 7.8 Homo sapiens
0.0017
-
beta-casein PDZ domain deletion mutant, K0.5 value, Hill constant 1.4, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
0.0017
-
beta-casein PDZ domain deletion mutant, K0.5 value, Hill constant 1.5, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
0.0018
-
beta-casein PDZ domain deletion mutant, K0.5 value, Hill constant 1.5, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
0.0023
-
beta-casein wild-type, K0.5 value, Hill constant 1.6, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
0.0023
-
beta-casein wild-type, K0.5 value, Hill constant 1.8, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
0.0023
-
beta-casein wild-type, K0.5 value, Hill constant 2.8, 37°C, pH 7.8 Homo sapiens
0.0027
-
beta-casein wild-type, K0.5 value, Hill constant 1.5, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
0.003
-
beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
0.0032
-
beta-casein mutant G230A, K0.5 value, 37°C, pH 7.8 Homo sapiens
0.0032
-
beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
0.0035
-
beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O43464
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
beta-casein + H2O
-
Homo sapiens ?
-
?

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.16
-
beta-casein mutant G230A, 37°C, pH 7.8 Homo sapiens
0.26
-
beta-casein mutant G230A, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
0.29
-
beta-casein PDZ domain deletion mutant, Hill constant 1.7, 37°C, pH 7.8 Homo sapiens
0.44
-
beta-casein mutant G230A, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
0.51
-
beta-casein mutant G230A, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
0.51
-
beta-casein PDZ domain deletion mutant, Hill constant 1.5, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
0.62
-
beta-casein PDZ domain deletion mutant, Hill constant 1.4, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
0.8
-
beta-casein PDZ domain deletion mutant, Hill constant 1.5, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
1.6
-
beta-casein wild-type, Hill constant 2.8, 37°C, pH 7.8 Homo sapiens
3.1
-
beta-casein wild-type, Hill constant 1.8, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
3.8
-
beta-casein wild-type, Hill constant 1.6, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
4.7
-
beta-casein wild-type, Hill constant 1.5, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens