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Literature summary extracted from

  • Balzarini, J.; Degreve, B.; Hatse, S.; De Clercq, E.; Breuer, M.; Johansson, M.; Huybrechts, R.; Karlsson, A.
    The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides (2000), Mol. Pharmacol., 57, 811-819.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.1.145 agriculture multifunctional deoxynucleoside kinase of insect cells is a target for development of new highly selective insecticidial drugs Drosophila melanogaster

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.1.145 wild-type and mutant enzymes, expression in Escherichia coli Drosophila melanogaster

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.145 (E)-5-(2-bromovinyl)-2'-deoxyuridine
-
Drosophila melanogaster
2.7.1.145 (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-monophosphate IC50: 0.0026 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster
2.7.1.145 (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate IC50: 0.0069 mM, reaction with thymidine, fusion protein with glutathione S-transferase. The inhibitor is efficiently metabolized to its 5'-mono-, 5'-di- and 5'-triphosphate derivatives in the insect cell culture and abundently incorporated into the insect cell DNA Drosophila melanogaster
2.7.1.145 dTTP IC50: 0.012 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster
2.7.1.145 additional information multifunctional deoxynucleoside kinase of insect cells is a target for development of new highly selective insecticidial drugs Drosophila melanogaster

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.1.145 0.0045
-
(E)-5-(2-bromovinyl)-2'-deoxyuridine 37°C, fusion protein with glutathione S-transferase Drosophila melanogaster

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.145 thymidine + ATP Drosophila melanogaster
-
thymidine 5'-phosphate + ADP
-
?

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
-
Drosophila melanogaster (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate + ADP
-
?
2.7.1.145 thymidine + ATP
-
Drosophila melanogaster thymidine 5'-phosphate + ADP
-
?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.145 0.00066
-
(E)-5-(2-bromovinyl)-2'-deoxyuridine pH 7.6, 30°C, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.1.145 0.0026
-
IC50: 0.0026 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-monophosphate
2.7.1.145 0.0069
-
IC50: 0.0069 mM, reaction with thymidine, fusion protein with glutathione S-transferase. The inhibitor is efficiently metabolized to its 5'-mono-, 5'-di- and 5'-triphosphate derivatives in the insect cell culture and abundently incorporated into the insec Drosophila melanogaster (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate
2.7.1.145 0.012
-
IC50: 0.012 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster dTTP