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Literature summary extracted from

  • Murakami, E.; Niu, C.; Bao, H.; Micolochick Steuer, H.M.; Whitaker, T.; Nachman, T.; Sofia, M.A.; Wang, P.; Otto, M.J.; Furman, P.A.
    The mechanism of action of beta-D-2-deoxy-2-fluoro-2-C-methylcytidine involves a second metabolic pathway leading to beta-D-2-deoxy-2-fluoro-2-C-methyluridine 5-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase (2008), Antimicrob. Agents Chemother., 52, 458-464.
    View publication on PubMedView publication on EuropePMC

Protein Variants

EC Number Protein Variants Comment Organism
2.7.7.48 S282T the mutation shows reduced sensitivity to 2'-hydroxy-2'-C-methyl nucleosides Hepacivirus C

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.48 beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate PSI-6130-TP, potent inhibitor Hepacivirus C
2.7.7.48 beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate also named RO2433-TP or PSI-6206, potent inhibitor Hepacivirus C

Organism

EC Number Organism UniProt Comment Textmining
2.7.7.48 Hepacivirus C
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.7.48 nucleoside triphosphate + RNAn
-
 Hepacivirus C diphosphate + RNAn+1
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.7.48 NS5B protein
-
 Hepacivirus C
2.7.7.48 RDRP
-
 Hepacivirus C
2.7.7.48 RNA-dependent RNA polymerase
-
 Hepacivirus C

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.7.48 0.000059
-
 beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate wild type enzyme, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
2.7.7.48 0.00022
-
 beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate mutant enzyme S282T, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
2.7.7.48 0.00031
-
 beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine 5'-triphosphate mutant enzyme S282T, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C
2.7.7.48 0.00042
-
 beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate wild type enzyme, with 5 mM MgCl2, and 2 mM dithiothreitol in 50 mM HEPES buffer, pH 7.5 Hepacivirus C