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Literature summary 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

Protein Variants

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.74 0.001
-
 deoxycytidine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.001
-
 deoxycytidine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.00104
-
 deoxycytidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.00141
-
 deoxycytidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.00154
-
 deoxycytidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.002
-
 deoxycytidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.00388
-
 thymidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.00455
-
 deoxycytidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.00525
-
 deoxycytidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.00558
-
 thymidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.0058
-
 thymidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.0086
-
 deoxycytidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.0118
-
 deoxycytidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.0189
-
 thymidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.0209
-
 deoxycytidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.025
-
 thymidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.0256
-
 thymidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.0257
-
 thymidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.031
-
 thymidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.036
-
 thymidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.071
-
 deoxycytidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.074
-
 thymidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.079
-
 2'-deoxyguanosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.081
-
 2'-deoxyadenosine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.081
-
 2'-deoxyadenosine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.081
-
 2'-deoxyguanosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.091
-
 2'-deoxyadenosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.154
-
 2'-deoxyguanosine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.155
-
 2'-deoxyguanosine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.231
-
 2'-deoxyadenosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.24
-
 2'-deoxyguanosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.324
-
 2'-deoxyguanosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.398
-
 2'-deoxyadenosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.412
-
 2'-deoxyadenosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.452
-
 2'-deoxyadenosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.532
-
 2'-deoxyadenosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.598
-
 2'-deoxyadenosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.691
-
 2'-deoxyadenosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.739
-
 2'-deoxyguanosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.843
-
 2'-deoxyadenosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.164
-
 2'-deoxyguanosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.172
-
 2'-deoxyguanosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.203
-
 2'-deoxyguanosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.28
-
 2'-deoxyguanosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.364
-
 2'-deoxyguanosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.437
-
 2'-deoxyadenosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.485
-
 thymidine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.485
-
 thymidine wild-type, pH 7.5, 30°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.74 Homo sapiens P27707
-
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.7.1.74 6.5
-
 substrate dideoxythymidine, wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 26
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 28
-
 substrate dideoxythymidine, mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 64
-
 substrate dideoxythymidine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 88
-
 substrate 2'-deoxy-3'-thiacytidine, wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 108
-
 substrate dideoxythymidine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 114
-
 substrate 2'-deoxy-3'-thiacytidine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 135
-
 substrate dideoxythymidine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 149
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 186
-
 substrate dideoxythymidine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 206
-
 substrate dideoxythymidine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
2.7.1.74 270
-
 substrate 2'-deoxy-3'-thiacytidine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 545
-
 substrate 2'-deoxy-3'-thiacytidine, mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 599
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 815
-
 substrate 2'-deoxy-3'-thiacytidine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
2.7.1.74 984
-
 substrate 1-beta-D-arabinosylcytosine, wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 1387
-
 substrate 1-beta-D-arabinosylcytosine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 1648
-
 substrate gemcitabine, wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 2262
-
 substrate gemcitabine, mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 3177
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 3308
-
 substrate 1-beta-D-arabinosylcytosine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 3339
-
 substrate 1-beta-D-arabinosylcytosine, mutant R104M/D133SA, pH 7.5, 37°C Homo sapiens
2.7.1.74 4267
-
 substrate gemcitabine, mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 4400
-
 substrate 1-beta-D-arabinosylcytosine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens
2.7.1.74 4530
-
 substrate gemcitabine, mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 5624
-
 substrate gemcitabine, mutant R104M/D133SA, pH 7.5, 37°C Homo sapiens
2.7.1.74 6009
-
 substrate gemcitabine, mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 6460
-
 substrate gemcitabine, mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 37°C Homo sapiens

Substrates and Products (Substrate)

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.74 0.064
-
 deoxycytidine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.064
-
 deoxycytidine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.21
-
 deoxycytidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.31
-
 2'-deoxyguanosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.37
-
 deoxycytidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.38
-
 thymidine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.38
-
 thymidine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 0.58
-
 deoxycytidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 0.68
-
 thymidine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.01
-
 thymidine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.08
-
 2'-deoxyadenosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.18
-
 2'-deoxyguanosine mutant D47E/R104Q/D133G/N163I/F242L, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.2
-
 deoxycytidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.23
-
 2'-deoxyguanosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.3
-
 deoxycytidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.49
-
 thymidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.5
-
 2'-deoxyguanosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.51
-
 thymidine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.57
-
 thymidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.7
-
 deoxycytidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.72
-
 2'-deoxyguanosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.75
-
 2'-deoxyadenosine mutant R104Q/D133G, pH 7.5, 30°C Homo sapiens
2.7.1.74 1.88
-
 thymidine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.91
-
 thymidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 1.92
-
 2'-deoxyguanosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 2
-
 2'-deoxyadenosine mutant R104Q/D133N, pH 7.5, 30°C Homo sapiens
2.7.1.74 2.1
-
 deoxycytidine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.23
-
 deoxycytidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.27
-
 thymidine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.29
-
 2'-deoxyguanosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.33
-
 thymidine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.5
-
 2'-deoxyguanosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.67
-
 2'-deoxyadenosine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.71
-
 2'-deoxyadenosine mutant R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 2.86
-
 deoxycytidine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.1
-
 2'-deoxyadenosine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.1
-
 2'-deoxyadenosine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 3.26
-
 2'-deoxyguanosine wild-type, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.26
-
 2'-deoxyguanosine wild-type, pH 7.5, 30°C Homo sapiens
2.7.1.74 3.29
-
 thymidine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.37
-
 2'-deoxyadenosine mutant A100V/R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.4
-
 2'-deoxyadenosine mutant A100V/R104M/D133A, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.47
-
 2'-deoxyadenosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.54
-
 deoxycytidine mutant A100V/R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 3.59
-
 2'-deoxyguanosine mutant R104M/D133N, pH 7.5, 37°C Homo sapiens
2.7.1.74 4.14
-
 2'-deoxyadenosine mutant R104M/D133T, pH 7.5, 37°C Homo sapiens
2.7.1.74 4.38
-
 2'-deoxyguanosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens
2.7.1.74 4.85
-
 2'-deoxyadenosine mutant R104M/D133S, pH 7.5, 37°C Homo sapiens