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Literature summary for 2.7.1.74 extracted from

  • Iyidogan, P.; Lutz, S.
    Systematic exploration of active site mutations on human deoxycytidine kinase substrate specificity (2008), Biochemistry, 47, 4711-4720.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.74

Protein Variants

Protein Variants Comment Organism
A100V/R104M/D133A 12fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
A100V/R104M/D133S 6fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
A100V/R104M/D133T ratio kcat/Km for deoxycytidine similar to wild-type Homo sapiens
D47E/R104Q/D133G/N163I/F242L 1.5fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
additional information R104 and D133 are key residues for substrate specificity Homo sapiens
R104M/D133A 4fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
R104M/D133N 3fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
R104M/D133S 6fold increase in ratio kcat/Km for deoxycytidine Homo sapiens
R104M/D133T mutant with reversed substrate specificity, with elevated specific constant for thymidine phosphorylation and decreased activity for deeoxycytidine, deoxyadenosine, and deoxyguanosine Homo sapiens
R104Q/D133G mutant is a generalist kinase with broader specificity and elevated turnover compared with wild-type Homo sapiens
R104Q/D133N 1.5fold increase in ratio kcat/Km for deoxycytidine Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.001
-
 deoxycytidine wild-type, pH 7.5, 37°C Homo sapiens
0.001
-
 deoxycytidine wild-type, pH 7.5, 30°C Homo sapiens
0.00104
-
 deoxycytidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
0.00141
-
 deoxycytidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
0.00154
-
 deoxycytidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
0.002
-
 deoxycytidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
0.00388
-
 thymidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
0.00455
-
 deoxycytidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
0.00525
-
 deoxycytidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
0.00558
-
 thymidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
0.0058
-
 thymidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
0.0086
-
 deoxycytidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
0.0118
-
 deoxycytidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
0.0189
-
 thymidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
0.0209
-
 deoxycytidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
0.025
-
 thymidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
0.0256
-
 thymidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
0.0257
-
 thymidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
0.031
-
 thymidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
0.036
-
 thymidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
0.071
-
 deoxycytidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
0.074
-
 thymidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
0.079
-
 2'-deoxyguanosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
0.081
-
 2'-deoxyadenosine wild-type, pH 7.5, 37°C Homo sapiens
0.081
-
 2'-deoxyadenosine wild-type, pH 7.5, 30°C Homo sapiens
0.081
-
 2'-deoxyguanosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
0.091
-
 2'-deoxyadenosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
0.154
-
 2'-deoxyguanosine wild-type, pH 7.5, 37°C Homo sapiens
0.155
-
 2'-deoxyguanosine wild-type, pH 7.5, 30°C Homo sapiens
0.231
-
 2'-deoxyadenosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
0.24
-
 2'-deoxyguanosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
0.324
-
 2'-deoxyguanosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
0.398
-
 2'-deoxyadenosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
0.412
-
 2'-deoxyadenosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
0.452
-
 2'-deoxyadenosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
0.532
-
 2'-deoxyadenosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
0.598
-
 2'-deoxyadenosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
0.691
-
 2'-deoxyadenosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
0.739
-
 2'-deoxyguanosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
0.843
-
 2'-deoxyadenosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
1.164
-
 2'-deoxyguanosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
1.172
-
 2'-deoxyguanosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
1.203
-
 2'-deoxyguanosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
1.28
-
 2'-deoxyguanosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
1.364
-
 2'-deoxyguanosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
1.437
-
 2'-deoxyadenosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
3.485
-
 thymidine wild-type, pH 7.5, 37°C Homo sapiens
3.485
-
 thymidine wild-type, pH 7.5, 30°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27707
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
6.5
-
 substrate dideoxythymidine, wild-type, pH 7.5, 37°C Homo sapiens
26
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
28
-
 substrate dideoxythymidine, mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
64
-
 substrate dideoxythymidine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
88
-
 substrate 2'-deoxy-3'-thiacytidine, wild-type, pH 7.5, 37°C Homo sapiens
108
-
 substrate dideoxythymidine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
114
-
 substrate 2'-deoxy-3'-thiacytidine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
135
-
 substrate dideoxythymidine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
149
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
186
-
 substrate dideoxythymidine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
206
-
 substrate dideoxythymidine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
270
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
545
-
 substrate 2'-deoxy-3'-thiacytidine, mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
599
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
815
-
 substrate 2'-deoxy-3'-thiacytidine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
984
-
 substrate 1-beta-D-arabinosylcytosine, wild-type, pH 7.5, 37°C Homo sapiens
1387
-
 substrate 1-beta-D-arabinosylcytosine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
1648
-
 substrate gemcitabine, wild-type, pH 7.5, 37°C Homo sapiens
2262
-
 substrate gemcitabine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
3177
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
3308
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
3339
-
 substrate 1-beta-D-arabinosylcytosine, mutant R104M/D133SA, pH 7.5, 37°C Homo sapiens
4267
-
 substrate gemcitabine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
4400
-
 substrate 1-beta-D-arabinosylcytosine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
4530
-
 substrate gemcitabine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
5624
-
 substrate gemcitabine, mutant R104M/D133SA, pH 7.5, 37°C Homo sapiens
6009
-
 substrate gemcitabine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
6460
-
 substrate gemcitabine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 1-beta-D-arabinosylcytosine
-
 Homo sapiens ADP + 1-beta-D-arabinosylcytosine 5'-phosphate
-
 ?
ATP + 2'-deoxy-3'-thiacytidine
-
 Homo sapiens ADP + 2'-deoxy-3'-thiacytidine 5'-phosphate
-
 ?
ATP + 2'-deoxyadenosine
-
 Homo sapiens ADP + 2'-deoxyadenosine 5'-phosphate
-
 ?
ATP + 2'-deoxycytidine
-
 Homo sapiens ADP + 2'-deoxycytidine 5'-phosphate
-
 ?
ATP + 2'-deoxyguanosine
-
 Homo sapiens ADP + 2'-deoxyguanosine 5'-phosphate
-
 ?
ATP + dideoxythymidine
-
 Homo sapiens ADP + dideoxythymidine 5'-phosphate
-
 ?
ATP + gemcitabine
-
 Homo sapiens ADP + gemcitabine 5'-phosphate
-
 ?
ATP + thymidine
-
 Homo sapiens ADP + TMP
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.064
-
 deoxycytidine wild-type, pH 7.5, 37°C Homo sapiens
0.064
-
 deoxycytidine wild-type, pH 7.5, 30°C Homo sapiens
0.21
-
 deoxycytidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
0.31
-
 2'-deoxyguanosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
0.37
-
 deoxycytidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
0.38
-
 thymidine wild-type, pH 7.5, 37°C Homo sapiens
0.38
-
 thymidine wild-type, pH 7.5, 30°C Homo sapiens
0.58
-
 deoxycytidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
0.68
-
 thymidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
1.01
-
 thymidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
1.08
-
 2'-deoxyadenosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
1.18
-
 2'-deoxyguanosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
1.2
-
 deoxycytidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
1.23
-
 2'-deoxyguanosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
1.3
-
 deoxycytidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
1.49
-
 thymidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
1.5
-
 2'-deoxyguanosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
1.51
-
 thymidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
1.57
-
 thymidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
1.7
-
 deoxycytidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
1.72
-
 2'-deoxyguanosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
1.75
-
 2'-deoxyadenosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
1.88
-
 thymidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
1.91
-
 thymidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
1.92
-
 2'-deoxyguanosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2
-
 2'-deoxyadenosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.1
-
 deoxycytidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.23
-
 deoxycytidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.27
-
 thymidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.29
-
 2'-deoxyguanosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.33
-
 thymidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.5
-
 2'-deoxyguanosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.67
-
 2'-deoxyadenosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.71
-
 2'-deoxyadenosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.86
-
 deoxycytidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
3.1
-
 2'-deoxyadenosine wild-type, pH 7.5, 37°C Homo sapiens
3.1
-
 2'-deoxyadenosine wild-type, pH 7.5, 30°C Homo sapiens
3.26
-
 2'-deoxyguanosine wild-type, pH 7.5, 37°C Homo sapiens
3.26
-
 2'-deoxyguanosine wild-type, pH 7.5, 30°C Homo sapiens
3.29
-
 thymidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
3.37
-
 2'-deoxyadenosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
3.4
-
 2'-deoxyadenosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
3.47
-
 2'-deoxyadenosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
3.54
-
 deoxycytidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
3.59
-
 2'-deoxyguanosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
4.14
-
 2'-deoxyadenosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
4.38
-
 2'-deoxyguanosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
4.85
-
 2'-deoxyadenosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens