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Literature summary for 2.7.1.145 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
Search for more literature for 2.7.1.145

Application

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

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
(E)-5-(2-bromovinyl)-2'-deoxyuridine
-
 Drosophila melanogaster
(E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-monophosphate IC50: 0.0026 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster
(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
dTTP IC50: 0.012 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster
additional information multifunctional deoxynucleoside kinase of insect cells is a target for development of new highly selective insecticidial drugs Drosophila melanogaster

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Drosophila melanogaster
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(E)-5-(2-bromovinyl)-2'-deoxyuridine + ATP
-
 Drosophila melanogaster (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate + ADP
-
 ?
thymidine + ATP
-
 Drosophila melanogaster thymidine 5'-phosphate + ADP
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
0.012
-
 IC50: 0.012 mM, reaction with thymidine, fusion protein with glutathione S-transferase Drosophila melanogaster dTTP