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Literature summary for 3.6.1.15 extracted from

  • Locatelli, G.A.; Gosselin, G.; Spadari, S.; Maga, G.
    Hepatitis C virus NS3 NTPase/helicase:different stereoselectivity in nucleoside triphosphate utilisation suggests that NTPase and helicase activities are coupled by a nucleotide-dependent rate limiting step (2001), J. Mol. Biol., 313, 683-694.
    View publication on PubMed

Application

Application Comment Organism
medicine considered attractive target for anti-hepatitis C virus chemoterapy Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
2',3'-didehydro-thymidine triphosphate competitive to ATP Hepacivirus C
2',3'-dideoxy-5-fluorocytidine triphosphate competitive to ATP Hepacivirus C
3'-azido-2',3'-dideoxythymidine triphosphate competitive to ATP Hepacivirus C
ATP
-
Hepacivirus C
dATP competitive to ATP Hepacivirus C
dCTP competitive to ATP Hepacivirus C
ddCTP competitive to ATP Hepacivirus C
ddTTP competitive to ATP Hepacivirus C
dGTP competitive to ATP Hepacivirus C
dTTP competitive to ATP Hepacivirus C
L-dATP competitive to ATP Hepacivirus C
L-dCTP competitive to ATP Hepacivirus C
L-ddCTP competitive to ATP Hepacivirus C
L-dTTP competitive to ATP Hepacivirus C

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.45
-
ATP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
0.54
-
ATP pH 7.5, 25°C, NTPase activity Hepacivirus C
0.8
-
2',3'-didehydro-thymidine triphosphate pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
0.8
-
L-dATP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
0.9
-
ddTTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
2.3
-
3'-azido-2',3'-dideoxythymidine triphosphate pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
2.4
-
dTTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
3.8
-
ddCTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
4
-
dCTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
6.9
-
dATP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
9.9
-
L-dCTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C
28
-
L-dTTP pH 7.5, 25°C, NTP hydrolysis-dependent helicase activity Hepacivirus C

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Hepacivirus C multifunctional protein, possessing protease, NTPase and helicase activities. These activities are essential for the virus life cycle ?
-
?

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2',3'-didehydro-thymidine triphosphate + H2O
-
Hepacivirus C 2',3'-didehydro-thymidine diphosphate + phosphate
-
?
3'-azido-2',3'-dideoxythymidine triphosphate + H2O
-
Hepacivirus C 3'-azido-2',3'-dideoxythymidine diphosphate + phosphate
-
?
ATP + H2O
-
Hepacivirus C ADP + phosphate
-
?
dATP + H2O
-
Hepacivirus C dADP + phosphate
-
?
dCTP + H2O
-
Hepacivirus C dCDP + phosphate
-
?
ddCTP + H2O
-
Hepacivirus C ddCDP + phosphate
-
?
ddTTP + H2O
-
Hepacivirus C ddTDP + phosphate
-
?
dTTP + H2O
-
Hepacivirus C TDP + phosphate
-
?
L-dATP + H2O
-
Hepacivirus C L-dADP + phosphate
-
?
L-dCTP + H2O
-
Hepacivirus C CDP + phosphate
-
?
L-dTTP + H2O
-
Hepacivirus C L-dTDP + phosphate
-
?
additional information multifunctional protein, possessing protease, NTPase and helicase activities. These activities are essential for the virus life cycle Hepacivirus C ?
-
?
additional information multifunctional protein, possessing protease, NTPase and helicase activities. Different stereoselectivity in nucleoside triphosphate utilisation suggests that NTPase and helicase activities are coupled by a nucleotide-dependent rate limiting step Hepacivirus C ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.54
-
ATP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
0.6
-
dATP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
0.6
-
2',3'-didehydro-thymidine triphosphate pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
1.2
-
ddTTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
1.2
-
L-dATP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
1.3
-
L-dTTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
1.5
-
L-dCTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
2.1
-
3'-azido-2',3'-dideoxythymidine triphosphate pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
2.3
-
L-ddCTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
2.5
-
2',3'-dideoxy-5-fluorocytidine triphosphate pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
2.8
-
dTTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
3
-
dCTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
3.5
-
dGTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C
3.8
-
ddCTP pH 7.5, 25°C, inhibition of ATPase activity Hepacivirus C