Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Poliakov, A.; Sandstroem, A.; Akerblom, E.; Danielson, U.H.
    Mechanistic studies of electrophilic protease inhibitors of full length hepatic C virus (HCV) NS3 (2007), J. Enzyme Inhib. Med. Chem., 22, 191-199.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.98 1-aminocyclopropane-1-carboxylic acid ketoacid electrophilic and acidic compound Hepacivirus C
3.4.21.98 1-aminocyclopropane-1-carboxylic acid ketotetrazole electrophilic and acidic compound Hepacivirus C
3.4.21.98 1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone electrophilic and non-acidic compound Hepacivirus C
3.4.21.98 1-aminocyclopropanecarboxylic acid non-electrophilic and acidic compound Hepacivirus C
3.4.21.98 L-aminobutyric acid carboxylic acid non-electrophilic and acidic compound Hepacivirus C
3.4.21.98 L-aminobutyric acid pentafluoroethyl ketone electrophilic and non-acidic compound Hepacivirus C
3.4.21.98 L-norvaline carboxylic acid non-electrophilic and acidic compound Hepacivirus C
3.4.21.98 L-norvaline ketotetrazole electrophilic and acidic compound Hepacivirus C
3.4.21.98 L-norvaline pentafluoroethyl ketone electrophilic and non-acidic compound Hepacivirus C
3.4.21.98 additional information electrophilic compounds with a pentafluoroethyl ketone group show stronger inhibition at pH 8 than pH 6, the difference is only significant at high ionic strength. Electrophilic compounds with an acidic C-terminal group or a cyclic P1 residue show a lower inhibitory effect at pH 8 than at pH 6, inconsistent with a mechanism-based inhibition. All electrophilic compounds have a strong inhibition at pH 6, when mechanism-based inhibition is unlikely Hepacivirus C

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.98 Ac-DED-(EDANS)-EEAbupsi[COO]ASK(Dabcyl)-NH2 + H2O
-
 Hepacivirus C ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.98 NS3
-
 Hepacivirus C
3.4.21.98 NS3 protease
-
 Hepacivirus C

Cofactor

EC Number Cofactor Comment Organism Structure
3.4.21.98 KKGSVVIVGRIVLSGK
-
 Hepacivirus C

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.98 0.0000062
-
 1-aminocyclopropanecarboxylic acid at pH 6.0 Hepacivirus C
3.4.21.98 0.000016
-
 L-norvaline carboxylic acid at pH 6.0 Hepacivirus C
3.4.21.98 0.000025
-
 1-aminocyclopropanecarboxylic acid at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.000031
-
 L-norvaline carboxylic acid at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.000051
-
 L-aminobutyric acid pentafluoroethyl ketone at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.000052
-
 1-aminocyclopropane-1-carboxylic acid ketoacid at pH 6.0 Hepacivirus C
3.4.21.98 0.000084
-
 L-aminobutyric acid pentafluoroethyl ketone at pH 6.0 Hepacivirus C
3.4.21.98 0.000098
-
 L-aminobutyric acid carboxylic acid at pH 6.0 Hepacivirus C
3.4.21.98 0.000117
-
 L-norvaline pentafluoroethyl ketone at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.000134
-
 L-norvaline ketotetrazole at pH 6.0 Hepacivirus C
3.4.21.98 0.000145
-
 L-norvaline pentafluoroethyl ketone at pH 8.0 Hepacivirus C
3.4.21.98 0.00015
-
 L-norvaline pentafluoroethyl ketone at pH 6.0 Hepacivirus C
3.4.21.98 0.00015
-
 L-aminobutyric acid pentafluoroethyl ketone at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00019
-
 1-aminocyclopropane-1-carboxylic acid ketoacid at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.0002
-
 1-aminocyclopropanecarboxylic acid at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.000245
-
 L-norvaline carboxylic acid at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00025
-
 L-aminobutyric acid carboxylic acid at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00032
-
 1-aminocyclopropanecarboxylic acid at pH 8.0 Hepacivirus C
3.4.21.98 0.00035
-
 L-norvaline pentafluoroethyl ketone at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00037
-
 1-aminocyclopropane-1-carboxylic acid ketotetrazole at pH 6.0 Hepacivirus C
3.4.21.98 0.00045
-
 L-norvaline carboxylic acid at pH 8.0 Hepacivirus C
3.4.21.98 0.00046
-
 L-norvaline ketotetrazole at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00082
-
 L-aminobutyric acid pentafluoroethyl ketone at pH 8.0 Hepacivirus C
3.4.21.98 0.00107
-
 1-aminocyclopropane-1-carboxylic acid ketotetrazole at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00125
-
 L-aminobutyric acid carboxylic acid at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00149
-
 1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone at pH 6.0 Hepacivirus C
3.4.21.98 0.00168
-
 1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00174
-
 L-norvaline ketotetrazole at pH 8.0 Hepacivirus C
3.4.21.98 0.00182
-
 1-aminocyclopropane-1-carboxylic acid ketoacid at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00188
-
 L-norvaline ketotetrazole at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00227
-
 1-aminocyclopropane-1-carboxylic acid ketotetrazole at pH 8.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00275
-
 L-aminobutyric acid carboxylic acid at pH 8.0 Hepacivirus C
3.4.21.98 0.0032
-
 1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone at pH 6.0 and 100 mM NaCl Hepacivirus C
3.4.21.98 0.00377
-
 1-aminocyclopropane-1-carboxylic acid ketoacid at pH 8.0 Hepacivirus C
3.4.21.98 0.0041
-
 1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone at pH 8.0 Hepacivirus C
3.4.21.98 0.00562
-
 1-aminocyclopropane-1-carboxylic acid ketotetrazole at pH 8.0 Hepacivirus C