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Literature summary for 3.4.21.98 extracted from

  • Lin, C.; Gates, C.A.; Rao, B.G.; Brennan, D.L.; Fulghum, J.R.; Luong, Y.P.; Frantz, J.D.; Lin, K.; Ma, S.; Wei, Y.Y.; Perni, R.B.; Kwong, A.D.
    In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061 (2005), J. Biol. Chem., 280, 36784-36791.
    View publication on PubMed
Search for more literature for 3.4.21.98

Protein Variants

Protein Variants Comment Organism
A156S resistant to inhibitor VX-950, sensitive to inhibitor BILN 2061 Hepacivirus C
A156T resistant to both inhibotors VX-950 and BILN 2061, diminished replication capacity in a transient replicon cell system Hepacivirus C
A156V resistant to both inhibotors VX-950 and BILN 2061, diminished replication capacity in a transient replicon cell system Hepacivirus C
D168A sensitive to inhibitor VX-950, resistant to inhibitor BILN 2061 Hepacivirus C
D168V sensitive to inhibitor VX-950, resistant to inhibitor BILN 2061 Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
BILN 2061
-
 Hepacivirus C
VX-950
-
 Hepacivirus C

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 wild-type, pH 7.8, 30°C Hepacivirus C
1.3
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 mutant A156T, pH 7.8, 30°C Hepacivirus C
2.6
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 mutant A156V, pH 7.8, 30°C Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C P26663
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 + H2O
-
 Hepacivirus C ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.2
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 mutant A156T, pH 7.8, 30°C Hepacivirus C
0.6
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 mutant A156V, pH 7.8, 30°C Hepacivirus C
1
-
 Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 wild-type, pH 7.8, 30°C Hepacivirus C

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000019
-
 BILN 2061 wild-type, pH 7.8, 30°C Hepacivirus C
0.0001
-
 VX-950 wild-type, pH 7.8, 30°C Hepacivirus C
0.0012
-
 BILN 2061 or above, mutant A156T, pH 7.8, 30°C Hepacivirus C
0.0012
-
 BILN 2061 or above, mutant A156V, pH 7.8, 30°C Hepacivirus C
0.0099
-
 VX-950 mutant A156T, pH 7.8, 30°C Hepacivirus C
0.033
-
 VX-950 mutant A156V, pH 7.8, 30°C Hepacivirus C