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Literature summary for 3.4.21.98 extracted from

  • Tong, X.; Guo, Z.; Wright-Minogue, J.; Xia, E.; Prongay, A.; Madison, V.; Qiu, P.; Venkatraman, S.; Velazquez, F.; Njoroge, F.G.; Malcolm, B.A.
    Impact of naturally occurring variants of HCV protease on the binding of different classes of protease inhibitors (2006), Biochemistry, 45, 1353-1361.
    View publication on PubMed
Search for more literature for 3.4.21.98

Protein Variants

Protein Variants Comment Organism
D168Q genotype 3 mutant, 30% decrease in Km-value Hepacivirus C
D79E genotype 2 mutant, 50% increase in Km-value Hepacivirus C
Q80G genotype 2 mutant, 50% increase in Km-value Hepacivirus C
R123T genotype 3 mutant, 40% increase in Km-value Hepacivirus C
R123T/D168Q genotype 3 mutant, slight decrease in Km-value Hepacivirus C
R123T/D168Q/V132L genotype 3 mutant, slight decrease in Km-value Hepacivirus C
S122K genotype 2 mutant, 30% increase in Km-value Hepacivirus C
S122K/V132L genotype 2 mutant, 2fold increase in Km-value Hepacivirus C
T160A genotype 2 mutant, 40% increase in Km-value Hepacivirus C
V132L genotype 2 and 3 mutant, 4fold decrease in kcat value Hepacivirus C
V78A genotype 2 mutant, 50% increase in Km-value Hepacivirus C
V78A/D79E/Q80G genotype 2 mutant, 3fold increase in Km-value Hepacivirus C
V78A/D79E/Q80G/S122K/V321L genotype 2 mutant, 2fold increase in Km-value Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
BILN 2061 significantly less active on genotype 2 and 3 enzyme Hepacivirus C
VX-950 equally active on enzyme from all three genotypes Hepacivirus C

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0012
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T, 30°C, pH 6.5 Hepacivirus C
0.0026
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 enzyme, 30°C, pH 6.5 Hepacivirus C
0.0034
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 and 3 mutant V132L, 30°C, pH 6.5 Hepacivirus C
0.0039
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 1b enzyme, 30°C, pH 6.5 Hepacivirus C
0.0042
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant D168Q, 30°C, pH 6.5 Hepacivirus C
0.0044
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant S122K/V132L, 30°C, pH 6.5 Hepacivirus C
0.0047
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A/D79E/Q80G/S122K/V321L, 30°C, pH 6.5 Hepacivirus C
0.0048
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant S122K, 30°C, pH 6.5 Hepacivirus C
0.005
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant T160A, 30°C, pH 6.5 Hepacivirus C
0.005
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T/D168Q/V132L, 30°C, pH 6.5 Hepacivirus C
0.0051
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T/D168Q, 30°C, pH 6.5 Hepacivirus C
0.0055
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant Q80G, 30°C, pH 6.5 Hepacivirus C
0.0058
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant D79E, 30°C, pH 6.5 Hepacivirus C
0.0059
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A, 30°C, pH 6.5 Hepacivirus C
0.0072
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 enzyme, 30°C, pH 6.5 Hepacivirus C
0.0073
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A/D79E/Q80G, 30°C, pH 6.5 Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C P27958
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester + H2O
-
 Hepacivirus C ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.033
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant D168Q, 30°C, pH 6.5 Hepacivirus C
0.095
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 and 3 mutant V132L, 30°C, pH 6.5 Hepacivirus C
0.13
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T, 30°C, pH 6.5 Hepacivirus C
0.133
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A/D79E/Q80G/S122K/V321L, 30°C, pH 6.5 Hepacivirus C
0.16
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A/D79E/Q80G, 30°C, pH 6.5 Hepacivirus C
0.2
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant T160A, 30°C, pH 6.5 Hepacivirus C
0.22
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant D79E, 30°C, pH 6.5 Hepacivirus C
0.22
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant Q80G, 30°C, pH 6.5 Hepacivirus C
0.25
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant S122K/V132L, 30°C, pH 6.5 Hepacivirus C
0.25
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T/D168Q, 30°C, pH 6.5 Hepacivirus C
0.3
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant V78A, 30°C, pH 6.5 Hepacivirus C
0.3
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 mutant R123T/D168Q/V132L, 30°C, pH 6.5 Hepacivirus C
0.4
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 1b enzyme, 30°C, pH 6.5 Hepacivirus C
0.43
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 enzyme, 30°C, pH 6.5 Hepacivirus C
0.57
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 3 enzyme, 30°C, pH 6.5 Hepacivirus C
0.58
-
 Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester genotype 2 mutant S122K, 30°C, pH 6.5 Hepacivirus C