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Literature summary for 3.4.21.98 extracted from

  • Massariol, M.J.; Zhao, S.; Marquis, M.; Thibeault, D.; White, P.W.
    Protease and helicase activities of hepatitis C virus genotype 4, 5, and 6 NS3-NS4A proteins (2010), Biochem. Biophys. Res. Commun., 391, 692-697.
    View publication on PubMed
Search for more literature for 3.4.21.98

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) and in Rosetta (DE3) cells Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
BILN 2061
-
 Hepacivirus C

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0013
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0021
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0028
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0035
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0066
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
 genotypes 1b, 2a, 4a, 5a, and 6a
-

Purification (Commentary)

Purification (Comment) Organism
nickel affinity resin column chromatography and poly-uridine affinity resin column chromatography Hepacivirus C

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Hepacivirus C
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH + H2O
-
 Hepacivirus C ?
-
 ?

Synonyms

Synonyms Comment Organism
NS3-NS4A protease
-
 Hepacivirus C

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.21
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.77
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.83
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.85
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
1.7
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
 BILN 2061 enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0000014
-
 BILN 2061 enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.000003
-
 BILN 2061 enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.0000037
-
 BILN 2061 enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
0.000015
-
 BILN 2061 enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000047
-
 enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C Hepacivirus C BILN 2061
0.0000048
-
 enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C BILN 2061
0.0000053
-
 enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C BILN 2061
0.0000102
-
 enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C BILN 2061
0.000037
-
 enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C BILN 2061

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
160
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
230
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
260
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
300
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C Hepacivirus C
370
-
 anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C Hepacivirus C