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Literature summary extracted from

  • Knecht, W.; Munch-Petersen, B.; Piskur, J.
    Identification of residues involved in the specificity and regulation of the highly efficient multisubstrate deoxyribonucleoside kinase from Drosophila melanogaster (2000), J. Mol. Biol., 301, 827-837.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
2.7.1.145 I102M/N117S/M118V/D208N clones harbouring the mutant enzyme are more sensitive to 3'-azido-2',3'-dideoxythymidine and beta-D-arabinofuranosylcytosine Drosophila melanogaster
2.7.1.145 I47T/N210D clones harbouring the mutant enzyme are more sensitive to 3'-azido-2',3'-dideoxythymidine and beta-D-arabinofuranosylcytosine Drosophila melanogaster
2.7.1.145 M1T/T85A/N121S clones harbouring the mutant enzyme are more sensitive to 1-beta-D-arabinofuranosylcytosine and 2',3'-dideoxycytidine Drosophila melanogaster
2.7.1.145 N210D/L239P clones harbouring the mutant enzyme are more sensitive to 3'-azido-2',3'-dideoxythymidine and beta-D-arabinofuranosylcytosine Drosophila melanogaster
2.7.1.145 N38D/N64D clones harbouring the mutant enzyme are more sensitive specifically to 3'-azido-2',3'-dideoxythymidine Drosophila melanogaster
2.7.1.145 N45D/N64D clones harbouring the mutant enzyme are more sensitive to 3'-azido-2',3'-dideoxythymidine and other nucleoside analogs Drosophila melanogaster
2.7.1.145 N45D/N64D mutant enzyme with the largest und universal increase in sensitivity of all mutants tested. 316fold increase to 3'-azido-2',3'-dideoxythymidine, more than 11fold to 2',3'-dideoxycytidine, and 3.2fold increase in sensitivity to beta-D-arabinofuranosylcytosine and 2',3'-dideoxyadenosine. Higher Km-values for native substrates than wild-type enzyme and Vmax-values are substantially lower, decrease in feedback inhibition by TTP, Km and Vmax values for 3'-azido-2',3'-dideoxythymidine and Km value for 2',3'-dideoxycytidine are nearly unchanged Drosophila melanogaster
2.7.1.145 N59D/M118V/Y179H clones harbouring the mutant enzyme are more sensitive to 3'-azido-2',3'-dideoxythymidine and beta-D-arabinofuranosylcytosine Drosophila melanogaster
2.7.1.145 N64S/L68S/M69L clones harbouring the mutant enzyme are more sensitive specifically to 3'-azido-2',3'-dideoxythymidine Drosophila melanogaster
2.7.1.145 T12A/V84A/N213S clones harbouring the mutant enzyme are more sensitive to 1-beta-D-arabinofuranosylcytosine Drosophila melanogaster
2.7.1.145 T85A clones harbouring the mutant enzyme are more sensitive to 1-beta-D-arabinofuranosylcytosine and 2',3'-dideoxycytidine Drosophila melanogaster
2.7.1.145 V84A clones harbouring the mutant enzyme are more sensitive to 1-beta-D-arabinofuranosylcytosine Drosophila melanogaster

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.145 TTP mutant enzyme N45D/N64D shows a decrease in feedback inhibition compared to the wild-type enzyme Drosophila melanogaster

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.145 0.0072
-
 3'-azido-2',3'-dideoxythymidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 0.0083
-
 3'-azido-2',3'-dideoxythymidine
-
 Drosophila melanogaster
2.7.1.145 0.0242
-
 thymidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 0.0964
-
 2'-deoxycytidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 1.093
-
 2',3'-dideoxycytidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 1.124
-
 2',3'-dideoxycytidine
-
 Drosophila melanogaster
2.7.1.145 2.004
-
 2'-deoxyguanosine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 3.16
-
 2'-deoxyadenosine mutant enzyme N45D/N64D Drosophila melanogaster

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.145 Drosophila melanogaster
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.145 (E)-5-(2-bromovinyl)-2'-deoxyuridine + ATP 54% of the activity with thymidine Drosophila melanogaster (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate + ADP
-
 ?
2.7.1.145 1-beta-D-arabinofuranosylcytosine + ATP 58.2% of the activity with thymidine Drosophila melanogaster 1-beta-D-arabinofuranosylcytosine 5'-phosphate + ADP
-
 ?
2.7.1.145 1-beta-D-arabinofuranosylthymine + ATP 53.9% of the activity with thymidine Drosophila melanogaster 1-beta-D-arabinofuranosylthymine 5'-phosphate + ADP
-
 ?
2.7.1.145 2',3'-dideoxyadenosine + ATP 0.9% of the activity with thymidine Drosophila melanogaster 2',3'-dideoxyadenosine 5'-phosphate + ADP
-
 ?
2.7.1.145 2',3'-dideoxycytidine + ATP
-
 Drosophila melanogaster 2',3'-dideoxycytidine 5'-phosphate + ADP
-
 ?
2.7.1.145 2'-deoxyadenosine + ATP
-
 Drosophila melanogaster 2'-deoxyadenosine 5'-phosphate + ADP
-
 ?
2.7.1.145 2'-deoxycytidine + ATP
-
 Drosophila melanogaster 2'-deoxycytidine 5'-phosphate + ADP
-
 ?
2.7.1.145 2'-deoxyguanosine + ATP
-
 Drosophila melanogaster 2'-deoxyguanosine 5'-phosphate + ADP
-
 ?
2.7.1.145 2'-deoxyuridine + ATP 113% of the activity with thymidine Drosophila melanogaster 2'-deoxyuridine 5'-phosphate + ADP
-
 ?
2.7.1.145 2-chloro-2'-deoxyadenosine + ATP 126% of the activity with thymidine Drosophila melanogaster 2-chloro-2'-deoxyadenosine 5'-phosphate + ADP
-
 ?
2.7.1.145 3'-azido-2',3'-dideoxythymidine + ATP
-
 Drosophila melanogaster 3'-azido-2',3'-dideoxythymidine 5'-phosphate + ADP
-
 ?
2.7.1.145 5-fluoro-2'-deoxyuridine + ATP 92% of the activity with thymidine Drosophila melanogaster 5-fluoro-2'-deoxyuridine 5'-phosphate + ADP
-
 ?
2.7.1.145 adenosine + ATP 0.82% of the activity with thymidine Drosophila melanogaster adenosine 5'-phosphate + ADP
-
 ?
2.7.1.145 cytidine + ATP 16% of the activity with thymidine Drosophila melanogaster cytidine 5'-phosphate + ADP
-
 ?
2.7.1.145 guanosine + ATP 1.18% of the activity with thymidine Drosophila melanogaster guanosine 5'-phosphate + ADP
-
 ?
2.7.1.145 thymidine + ATP
-
 Drosophila melanogaster thymidine 5'-phosphate + ADP
-
 ?
2.7.1.145 uridine + ATP 6.45% of the activity with thymidine Drosophila melanogaster uridine 5'-phosphate + ADP
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.1.145 0.036
-
 3'-azido-2',3'-dideoxythymidine
-
 Drosophila melanogaster
2.7.1.145 0.052
-
 3'-azido-2',3'-dideoxythymidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 0.076
-
 2'-deoxyguanosine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 0.54
-
 2',3'-dideoxycytidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 0.828
-
 2'-deoxyadenosine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 1.22
-
 thymidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 4.03
-
 2'-deoxycytidine mutant enzyme N45D/N64D Drosophila melanogaster
2.7.1.145 4.2
-
 2',3'-dideoxycytidine
-
 Drosophila melanogaster
2.7.1.145 14.2
-
 thymidine pH 7.8, 22°C, recombinant enzyme Drosophila melanogaster
2.7.1.145 15.1
-
 2'-deoxyguanosine pH 7.8, 22°C, recombinant enzyme Drosophila melanogaster
2.7.1.145 16.5
-
 2'-deoxycytidine pH 7.8, 22°C, recombinant enzyme Drosophila melanogaster
2.7.1.145 20.6
-
 2'-deoxyadenosine pH 7.8, 22°C, recombinant enzyme Drosophila melanogaster