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Literature summary 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

EC Number Activating Compound Comment Organism Structure
3.4.21.108 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
3.4.21.108 PDZ domain G230A mutation in recognition sequence of the PDZ domain, shows a significant decrease in the catalytic efficiency Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.108
-
 Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.4.21.108 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.108 0.0014
-
 beta-casein PDZ domain deletion mutant, K0.5 value, Hill constant 1.7, 37°C, pH 7.8 Homo sapiens
3.4.21.108 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
3.4.21.108 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
3.4.21.108 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
3.4.21.108 0.0023
-
 beta-casein wild-type, K0.5 value, Hill constant 2.8, 37°C, pH 7.8 Homo sapiens
3.4.21.108 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
3.4.21.108 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
3.4.21.108 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
3.4.21.108 0.003
-
 beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.0032
-
 beta-casein mutant G230A, K0.5 value, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.0032
-
 beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.0035
-
 beta-casein mutant G230A, K0.5 value, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.108 Homo sapiens O43464
-
-

Substrates and Products (Substrate)

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

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.4.21.108 0.16
-
 beta-casein mutant G230A, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.26
-
 beta-casein mutant G230A, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.29
-
 beta-casein PDZ domain deletion mutant, Hill constant 1.7, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.44
-
 beta-casein mutant G230A, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
3.4.21.108 0.51
-
 beta-casein mutant G230A, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens
3.4.21.108 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
3.4.21.108 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
3.4.21.108 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
3.4.21.108 1.6
-
 beta-casein wild-type, Hill constant 2.8, 37°C, pH 7.8 Homo sapiens
3.4.21.108 3.1
-
 beta-casein wild-type, Hill constant 1.8, presence of inhibitor of apoptosis domain BIR3, 37°C, pH 7.8 Homo sapiens
3.4.21.108 3.8
-
 beta-casein wild-type, Hill constant 1.6, presence of inhibitor of apoptosis domain BIR2, 37°C, pH 7.8 Homo sapiens
3.4.21.108 4.7
-
 beta-casein wild-type, Hill constant 1.5, presence of inhibitor of apoptosis protein, 37°C, pH 7.8 Homo sapiens