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Literature summary for 3.4.21.98 extracted from

  • Konstantinidis, A.K.; Richardson, P.L.; Kurtz, K.A.; Tripathi, R.; Chen, C.M.; Huang, P.; Randolph, J.; Towne, D.; Donnelly, J.; Warrior, U.; Middleton, T.; Kati, W.M.
    Longer wavelength fluorescence resonance energy transfer depsipeptide substrates for hepatitis C virus NS3 protease (2007), Anal. Biochem., 368, 156-167.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
recombinant single-chain NS3-4A protein containing an N-terminal hexahistidine tag expressed in Escherichia coli BL21(DE3) cells Hepacivirus C

Inhibitors

Inhibitors Comment Organism Structure
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
Hepacivirus C
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
Hepacivirus C
BILN-2061
-
Hepacivirus C

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0227
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide in the presence of 0.0174% DDM Hepacivirus C
0.03
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
Hepacivirus C
0.0367
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide operating at wavelengths 515 nm/605 nm (excitation/emission) Hepacivirus C
0.03984
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide operating at wavelengths 524 nm/600 nm (excitation/emission) Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
-
-

Purification (Commentary)

Purification (Comment) Organism
single-chain NS3-4A protein purified by gel filtration and on Ni2+-NTA fast flow column, more than 85% pure Hepacivirus C

Storage Stability

Storage Stability Organism
-80°C Hepacivirus C

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide + H2O
-
Hepacivirus C ?
-
?
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide + H2O efficient substrate for the protease Hepacivirus C ?
-
?

Synonyms

Synonyms Comment Organism
NS3 protease
-
Hepacivirus C
NS3-4A
-
Hepacivirus C

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.6
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
Hepacivirus C
1
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide operating at wavelengths 524 nm/600 nm (excitation/emission) Hepacivirus C
1.2
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide operating at wavelengths 515 nm/605 nm (excitation/emission) Hepacivirus C
7.2
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide in the presence of 0.0174% DDM Hepacivirus C

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000038
-
BILN-2061
-
Hepacivirus C
0.0002
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid with Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide as substrate Hepacivirus C
0.0003
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid with Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide as substrate Hepacivirus C
0.0038
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH for Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide Hepacivirus C
0.004
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH for AAc-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide Hepacivirus C