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Literature summary for 2.7.1.1 extracted from

  • Zelent, B.; Odili, S.; Buettger, C.; Zelent, D.K.; Chen, P.; Fenner, D.; Bass, J.; Stanley, C.; Laberge, M.; Vanderkooi, J.M.; Sarabu, R.; Grimsby, J.; Matschinsky, F.M.
    Mutational analysis of allosteric activation and inhibition of glucokinase (2011), Biochem. J., 440, 203-215.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli as a GST-fusion protein Homo sapiens

Protein Variants

Protein Variants Comment Organism
A379T kcat(1/sec): 61.2, D-glucose S05 (mM): 12.3, Km (ATP): 0.87 mM, relative inhibition of glucokinase activity through GKRP alone: 17% and GKRP plus 10 microM sorbitol 6-phosphate: 53% Homo sapiens
A456V kcat(1/sec): 65.6, D-glucose S05 (mM): 1.91, Km (ATP): 0.35 mM, relative inhibition of glucokinase activity through GKRP alone: 11% and GKRP plus 10 microM sorbitol 6-phosphate: 28% Homo sapiens
C213R kcat(1/sec): 50, D-glucose S05 (mM): 21.6, Km (ATP): 0.89 mM, relative inhibition of glucokinase activity through GKRP alone: 19% and GKRP plus 10 microM sorbitol 6-phosphate: 43% Homo sapiens
C252Y kcat(1/sec): 29.3, D-glucose S05 (mM): 31.6, Km (ATP): 0.75 mM, relative inhibition of glucokinase activity through GKRP alone: 4% and GKRP plus 10 microM sorbitol 6-phosphate: 4% Homo sapiens
E442K kcat(1/sec): 52.6, D-glucose S05 (mM): 5.24, Km (ATP): 1.5 mM, relative inhibition of glucokinase activity through GKRP alone: 14% and GKRP plus 10 microM sorbitol 6-phosphate: 40% Homo sapiens
G68K kcat(1/sec): 43.2, D-glucose S05 (mM): 2.34, Km (ATP): 0.39 mM, relative inhibition of glucokinase activity through GKRP alone: 2% and GKRP plus 10 microM sorbitol 6-phosphate: 20.5% Homo sapiens
G68V kcat(1/sec): 62.7, D-glucose S05 (mM): 2.2, Km (ATP): 0.31 mM, relative inhibition of glucokinase activity through GKRP alone: 15% and GKRP plus 10 microM sorbitol 6-phosphate: 32.5% Homo sapiens
G72R kcat(1/sec): 29.8, D-glucose S05 (mM): 7.38, Km (ATP): 0.72 mM, relative inhibition of glucokinase activity through GKRP alone: 5% and GKRP plus 10 microM sorbitol 6-phosphate: 6.5% Homo sapiens
K140E kcat(1/sec): 40, D-glucose S05 (mM): 10.8, Km (ATP): 0.35 mM, relative inhibition of glucokinase activity through GKRP alone: 9% and GKRP plus 10 microM sorbitol 6-phosphate: 10.5% Homo sapiens
K414E kcat(1/sec): 19.9, D-glucose S05 (mM): 5.69, Km (ATP): 1.53 mM, relative inhibition of glucokinase activity through GKRP alone: 13.5% and GKRP plus 10 microM sorbitol 6-phosphate: 49% Homo sapiens
M197E kcat(1/sec): 17.7, D-glucose S05 (mM): 41.6, Km (ATP): 0.4 mM, relative inhibition of glucokinase activity through GKRP alone: 13.5% and GKRP plus 10 microM sorbitol 6-phosphate: 18.5% Homo sapiens
M197I kcat(1/sec): 58.1, D-glucose S05 (mM): 2.49, Km (ATP): 1.39 mM, relative inhibition of glucokinase activity through GKRP alone: 47% and GKRP plus 10 microM sorbitol 6-phosphate: 59% Homo sapiens
M197I/A397T kcat(1/sec): 50.2, D-glucose S05 (mM): 5.81, Km (ATP): 2.71 mM, relative inhibition of glucokinase activity through GKRP alone: 18% and GKRP plus 10 microM sorbitol 6-phosphate: 37% Homo sapiens
M197L kcat(1/sec): 62.6, D-glucose S05 (mM): 4.03, Km (ATP): 1.31 mM, relative inhibition of glucokinase activity through GKRP alone: 15% and GKRP plus 10 microM sorbitol 6-phosphate: 37% Homo sapiens
M298K kcat(1/sec): 37.7, D-glucose S05 (mM): 10.8, Km (ATP): 3.32 mM, relative inhibition of glucokinase activity through GKRP alone: 20% and GKRP plus 10 microM sorbitol 6-phosphate: 44% Homo sapiens
P417R kcat(1/sec): 48.3, D-glucose S05 (mM): 6.59, Km (ATP): 2.08 mM, relative inhibition of glucokinase activity through GKRP alone: 10% and GKRP plus 10 microM sorbitol 6-phosphate: 39% Homo sapiens
S263P kcat(1/sec): 44.6, D-glucose S05 (mM): 9.7, Km (ATP): 0.63 mM, relative inhibition of glucokinase activity through GKRP alone: 19% and GKRP plus 10 microM sorbitol 6-phosphate: 49.5% Homo sapiens
S336L kcat(1/sec): 2.46, D-glucose S05 (mM): 4.75, Km (ATP): 12.6 mM Homo sapiens
S64P kcat(1/sec): 83.3, D-glucose S05 (mM): 2.07, Km (ATP): 0.32 mM, relative inhibition of glucokinase activity through GKRP alone: 5% and GKRP plus 10 microM sorbitol 6-phosphate: 4% Homo sapiens
S64Y kcat(1/sec): 114, D-glucose S05 (mM): 1.89, Km (ATP): 1.59 mM, relative inhibition of glucokinase activity through GKRP alone: 19% and GKRP plus 10 microM sorbitol 6-phosphate: 15% Homo sapiens
T65I kcat(1/sec): 22.6, D-glucose S05 (mM): 1.69, Km (ATP): 0.57 mM, relative inhibition of glucokinase activity through GKRP alone: 7.5% and GKRP plus 10 microM sorbitol 6-phosphate: 23% Homo sapiens
V389L kcat(1/sec): 67.1, D-glucose S05 (mM): 3.45, Km (ATP): 0.76 mM, relative inhibition of glucokinase activity through GKRP alone: 67% and GKRP plus 10 microM sorbitol 6-phosphate: 75% Homo sapiens
V452L kcat(1/sec): 122, D-glucose S05 (mM): 2.27, Km (ATP): 0.53 mM, relative inhibition of glucokinase activity through GKRP alone: 19% and GKRP plus 10 microM sorbitol 6-phosphate: 38% Homo sapiens
V455M kcat(1/sec): 61.8, D-glucose S05 (mM): 3.24, Km (ATP): 0.38 mM, relative inhibition of glucokinase activity through GKRP alone: 26% and GKRP plus 10 microM sorbitol 6-phosphate: 52% Homo sapiens
V62M kcat(1/sec): 47.2, D-glucose S05 (mM): 5.9, Km (ATP): 0.52 mM, relative inhibition of glucokinase activity through GKRP alone: 8.5% and GKRP plus 10 microM sorbitol 6-phosphate: 11.5% Homo sapiens
V91L kcat(1/sec): 60.6, D-glucose S05 (mM): 1.66, Km (ATP): 0.48 mM, relative inhibition of glucokinase activity through GKRP alone: 6% and GKRP plus 10 microM sorbitol 6-phosphate: 22.5% Homo sapiens
Y214A kcat(1/sec): 117, D-glucose S05 (mM): 1.41, Km (ATP): 0.92 mM, relative inhibition of glucokinase activity through GKRP alone: 24% and GKRP plus 10 microM sorbitol 6-phosphate: 53% Homo sapiens
Y214A/V452A kcat(1/sec): 23.1, D-glucose S05 (mM): 0.55, Km (ATP): 1.42 mM, relative inhibition of glucokinase activity through GKRP alone: 11.5% and GKRP plus 10 microM sorbitol 6-phosphate: 20% Homo sapiens
Y214C kcat(1/sec): 65.3, D-glucose S05 (mM): 1.35, Km (ATP): 1.08 mM, relative inhibition of glucokinase activity through GKRP alone: 19% and GKRP plus 10 microM sorbitol 6-phosphate: 41% Homo sapiens
Y215A kcat(1/sec): 44.7, D-glucose S05 (mM): 2.07, Km (ATP): 0.58 mM, relative inhibition of glucokinase activity through GKRP alone: 6% and GKRP plus 10 microM sorbitol 6-phosphate: 4.5% Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
glucokinase-regulatory protein GK regulatory protein, relative inhibition of glucokinase activity through GKRP alone wild-type: 32.5% and GKRP plus 10 microM sorbitol 6-phosphate: 55 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.31
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant 454-Ala Homo sapiens
0.31
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G68V Homo sapiens
0.32
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S64P Homo sapiens
0.35
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant A456V Homo sapiens
0.35
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant K140E Homo sapiens
0.38
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V455M Homo sapiens
0.39
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G68K Homo sapiens
0.4
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197E Homo sapiens
0.46
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, wild-type Homo sapiens
0.48
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V91L Homo sapiens
0.52
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V62M Homo sapiens
0.53
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V452L Homo sapiens
0.57
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant T65I Homo sapiens
0.58
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y215A Homo sapiens
0.63
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S263P Homo sapiens
0.72
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G72R Homo sapiens
0.75
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant C252Y Homo sapiens
0.76
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V389L Homo sapiens
0.87
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant A379T Homo sapiens
0.89
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant C213R Homo sapiens
0.92
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214A Homo sapiens
1.08
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214C Homo sapiens
1.31
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197L Homo sapiens
1.39
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197I Homo sapiens
1.42
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214A/V452A Homo sapiens
1.5
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant E442K Homo sapiens
1.53
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant K414E Homo sapiens
1.59
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S64Y Homo sapiens
2.08
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant P417R Homo sapiens
2.71
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197I/A379T Homo sapiens
3.32
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M298K Homo sapiens
12.6
-
ATP pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S336L Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P35557
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + D-glucose
-
Homo sapiens ADP + D-glucose 6-phosphate
-
?

Synonyms

Synonyms Comment Organism
glucokinase 1
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.46
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S336L Homo sapiens
17.7
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197E Homo sapiens
19.9
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant K414E Homo sapiens
22.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant T65I Homo sapiens
23.1
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214A/V452A Homo sapiens
29.3
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant C252Y Homo sapiens
29.8
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G72R Homo sapiens
37.7
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M298K Homo sapiens
40
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant K140E Homo sapiens
43.2
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G68K Homo sapiens
44.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S263P Homo sapiens
44.7
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y215A Homo sapiens
47.2
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V62M Homo sapiens
48.3
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant P417R Homo sapiens
50
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant C213R Homo sapiens
50.2
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197I/A379T Homo sapiens
52.2
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant 454-Ala Homo sapiens
52.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant E442K Homo sapiens
58.1
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197I Homo sapiens
60.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V91L Homo sapiens
61.2
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant A379T Homo sapiens
61.8
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V455M Homo sapiens
62.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant M197L Homo sapiens
62.7
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant G68V Homo sapiens
62.8
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, wild-type Homo sapiens
65.3
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214C Homo sapiens
65.6
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant A456V Homo sapiens
67.1
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V389L Homo sapiens
83.3
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S64P Homo sapiens
114
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant S64Y Homo sapiens
117
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant Y214A Homo sapiens
122
-
D-glucose pH 7.1, temperature not specified in the publication, co-substrate: ATP, mutant V452L Homo sapiens