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Literature summary for 3.4.11.6 extracted from

  • Ogawa, Y.; Ohnishi, A.; Goto, Y.; Sakuma, Y.; Watanabe, J.; Hattori, A.; Tsujimoto, M.
    Role of glutamine-169 in the substrate recognition of human aminopeptidase B (2014), Biochim. Biophys. Acta, 1840, 1872-1881.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
Q169E mutant shows no activity Homo sapiens
Q169N mutant shows a significant decrease in hydrolytic activity toward the fluorescent substrate Lys-4-methylcoumaryl-7-amide (MCA). Mutant shows an increase in IC50 values of inhibitors that interact with the catalytic pocket of aminopeptidase B. Km (Arg 4-methylcoumarin 7-amide) similar to wild-type, kcat (Arg 4-methylcoumarin 7-amide) decreased compared to wild-type. Km (Lys 4-methylcoumarin 7-amide) increased compared to wild-type, kcat (Lys 4-methylcoumarin 7-amide) decreased compared to wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,10-phenanthroline
-
Homo sapiens
arphamenine A
-
Homo sapiens
Arphamenine B
-
Homo sapiens
bestatin
-
Homo sapiens
kallidin human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 73.7% (wild-type enzyme) Homo sapiens
Substance P human peptide hormone, 100 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 63.8% (wild-type enzyme); human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 78% (wild-type enzyme) Homo sapiens
ZnCl2
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0157
-
kallidin pH 7.4, 37°C, wild-type Homo sapiens
0.021
-
Arg-Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
0.0251
-
Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
0.0533
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens
0.0651
-
kallidin pH 7.4, 37°C, mutant Q169N Homo sapiens
0.0774
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens
0.111
-
Arg-Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
0.36
-
Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
0.381
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens
0.568
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg 4-methylcoumarin 7-amide + H2O
-
Homo sapiens Arg + 7-amino-4-methylcoumarin
-
?
Arg-Met-enkephalin + H2O
-
Homo sapiens ?
-
?
kallidin + H2O
-
Homo sapiens ?
-
?
Lys 4-methylcoumarin 7-amide + H2O
-
Homo sapiens Lys + 7-amino-4-methylcoumarin
-
?
Met-enkephalin + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
aminopeptidase B
-
Homo sapiens
APB
-
Homo sapiens

Temperature Optimum [°C]

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

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.47
-
Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
0.48
-
Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
1.07
-
Arg-Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
1.95
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens
1.99
-
kallidin pH 7.4, 37°C, mutant Q169N Homo sapiens
2.35
-
kallidin pH 7.4, 37°C, wild-type Homo sapiens
3.63
-
Arg-Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
4.06
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens
9.27
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens
14.9
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000072
-
pH 7.4, 37°C, wild-type Homo sapiens Arphamenine B
0.00000155
-
pH 7.4, 37°C, mutant Q169N Homo sapiens Arphamenine B
0.00000316
-
pH 7.4, 37°C, mutant Q169N Homo sapiens arphamenine A
0.00000349
-
pH 7.4, 37°C, wild-type Homo sapiens bestatin
0.00000373
-
pH 7.4, 37°C, wild-type Homo sapiens arphamenine A
0.00000391
-
pH 7.4, 37°C, wild-type Homo sapiens ZnCl2
0.00000592
-
pH 7.4, 37°C, mutant Q169N Homo sapiens ZnCl2
0.00006
-
pH 7.4, 37°C, mutant Q169N Homo sapiens 1,10-phenanthroline
0.000077
-
pH 7.4, 37°C, wild-type Homo sapiens 1,10-phenanthroline
0.000289
-
pH 7.4, 37°C, mutant Q169N Homo sapiens bestatin

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1
-
Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
10.4
-
Arg-Met-enkephalin pH 7.4, 37°C, mutant Q169N Homo sapiens
19
-
Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
30.1
-
kallidin pH 7.4, 37°C, mutant Q169N Homo sapiens
156
-
kallidin pH 7.4, 37°C, wild-type Homo sapiens
173
-
Arg-Met-enkephalin pH 7.4, 37°C, wild-type Homo sapiens
3440
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens
39200
-
Lys 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens
52400
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, mutant Q169N Homo sapiens
175000
-
Arg 4-methylcoumarin 7-amide pH 7.4, 37°C, wild-type Homo sapiens