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Literature summary for 4.2.1.1 extracted from

  • Turkoglu, S.; Maresca, A.; Alper, M.; Kockar, F.; Isik, S.; Sinan, S.; Ozensoy, O.; Arslan, O.; Supuran, C.T.
    Mutation of active site residues Asn67 to Ile, Gln92 to Val and Leu204 to Ser in human carbonic anhydrase II: influences on the catalytic activity and affinity for inhibitors (2012), Bioorg. Med. Chem., 20, 2208-2213.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
L204S affinity for sulfonamides/sulfamate inhibitor is moderately decreased compared to wild-type. kcat and Km (CO2) comparable to wild-type Homo sapiens
N67I affinity for sulfonamides/sulfamate inhibitor is highly decreased compared to wild-type. kcat and Km (CO2) comparable to wild-type Homo sapiens
Q92V affinity for sulfonamides/sulfamate inhibitor is decreased compared to wild-type. kcat and Km (CO2) comparable to wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(1,2-benzoxazol-3-yl)methanesulfonamide
-
Homo sapiens
2-amino-1-benzothiophen-3(2H)-one 1,1-dioxide
-
Homo sapiens
4-(2-aminoethyl)benzenesulfonamide
-
Homo sapiens
4-(2-hydroxyethyl)benzenesulfonamide
-
Homo sapiens
4-amino-3-fluorobenzenesulfonamide
-
Homo sapiens
4-amino-6-chlorobenzene-1,3-disulfonamide
-
Homo sapiens
4-Aminobenzenesulfonamide
-
Homo sapiens
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
Homo sapiens
5-(formylamino)-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
5-amino-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
6-ethoxy-1,3-benzothiazole-2-sulfonamide
-
Homo sapiens
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
9
-
CO2 pH 7.5, 20°C, mutant N67I Homo sapiens
9.2
-
CO2 pH 7.5, 20°C, mutant Q92V Homo sapiens
9.3
-
CO2 pH 7.5, 20°C, wild-type Homo sapiens
9.3
-
CO2 pH 7.5, 20°C, mutant L204S Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CO2 + H2O
-
Homo sapiens H2CO3
-
?

Synonyms

Synonyms Comment Organism
hCAII
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
20
-
assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1000000
-
CO2 pH 7.5, 20°C, mutant Q92V Homo sapiens
1400000
-
CO2 pH 7.5, 20°C, wild-type Homo sapiens
1400000
-
CO2 pH 7.5, 20°C, mutant N67I Homo sapiens
1500000
-
CO2 pH 7.5, 20°C, mutant L204S Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000008
-
6-ethoxy-1,3-benzothiazole-2-sulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00001
-
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate wild-type, pH 7.5, 20°C Homo sapiens
0.000012
-
5-(formylamino)-1,3,4-thiadiazole-2-sulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.000021
-
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.000035
-
1-(1,2-benzoxazol-3-yl)methanesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00006
-
5-amino-1,3,4-thiadiazole-2-sulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00006
-
4-amino-3-fluorobenzenesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.000075
-
4-amino-6-chlorobenzene-1,3-disulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.000125
-
4-(2-hydroxyethyl)benzenesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00016
-
4-(2-aminoethyl)benzenesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00024
-
4-Aminobenzenesulfonamide wild-type, pH 7.5, 20°C Homo sapiens
0.00595
-
2-amino-1-benzothiophen-3(2H)-one 1,1-dioxide wild-type, pH 7.5, 20°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
108000
-
CO2 pH 7.5, 20°C, mutant Q92V Homo sapiens
150000
-
CO2 pH 7.5, 20°C, wild-type Homo sapiens
155000
-
CO2 pH 7.5, 20°C, mutant N67I Homo sapiens
161000
-
CO2 pH 7.5, 20°C, mutant L204S Homo sapiens