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Literature summary for 3.4.22.28 extracted from

  • Maugeri, C.; Alisi, M.A.; Apicella, C.; Cellai, L.; Dragone, P.; Fioravanzo, E.; Florio, S.; Furlotti, G.; Mangano, G.; Ombrato, R.; Luisi, R.; Pompei, R.; Rincicotti, V.; Russo, V.; Vitiello, M.; Cazzolla, N.
    New anti-viral drugs for the treatment of the common cold (2008), Bioorg. Med. Chem., 16, 3091-3107.
    View publication on PubMed

Application

Application Comment Organism
drug development 3CP is an optimal target for the development of anti-viral agents Human rhinovirus sp.

Inhibitors

Inhibitors Comment Organism Structure
3-(benzylamino)-5-[1-N-hydroxyethanimidoyl]benzamide
-
Human rhinovirus sp.
3-(bromoacetyl)-5-(naphth-2-ylmethyl)benzamide 12% inhibition at inhibitor concentration of 100 nM, 39% inhibition at inhibitor concentration of 1 microM, 83% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-(bromoacetyl)benzamide 4% inhibition at inhibitor concentration of 100 nM, 23% inhibition at inhibitor concentration of 1 microM, 85% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-(chloroacetyl)-5-(naphth-2-ylmethyl)benzamide 25% inhibition at inhibitor concentration of 100 nM, 61% inhibition at inhibitor concentration of 1 microM, 81% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-(chloroacetyl)benzamide
-
Human rhinovirus sp.
3-(dibromoacetyl)-5-(naphth-2-ylmethyl)benzamide
-
Human rhinovirus sp.
3-(dibromoacetyl)benzamide
-
Human rhinovirus sp.
3-(dichloroacetyl)benzamide
-
Human rhinovirus sp.
3-(difluoroacetyl)-5-[(phenylcarbonyl)amino]benzamide
-
Human rhinovirus sp.
3-(difluoroacetyl)benzamide
-
Human rhinovirus sp.
3-(trifluoroacetyl)benzamide no inhibition of 3CP Human rhinovirus sp.
3-(trifluoroacetyl)benzonitrile
-
Human rhinovirus sp.
3-acetyl-5-(5,8-dihydronaphthalen-2-ylmethyl)benzamide
-
Human rhinovirus sp.
3-acetyl-5-(naphth-1-ylcarbamoyl)benzoic acid
-
Human rhinovirus sp.
3-acetyl-5-(phenylcarbamoyl)benzoic acid
-
Human rhinovirus sp.
3-acetyl-5-benzylbenzamide
-
Human rhinovirus sp.
3-acetylbenzamide
-
Human rhinovirus sp.
3-benzyl-5-(bromoacetyl)benzamide 0% inhibition at inhibitor concentration of 100 nM, 30% inhibition at inhibitor concentration of 1 microM, 68% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-benzyl-5-(chloroacetyl)benzamide 14% inhibition at inhibitor concentration of 100 nM, 79% inhibition at inhibitor concentration of 1 microM, 91% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-benzyl-5-(dibromoacetyl)benzamide 14% inhibition at inhibitor concentration of 100 nM, 27% inhibition at inhibitor concentration of 1 microM, 75% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
3-benzyl-5-(difluoroacetyl)benzamide
-
Human rhinovirus sp.
4-(bromoacetyl)isoindolin-1-one
-
Human rhinovirus sp.
4-acetylisoindolin-1-one
-
Human rhinovirus sp.
4-bromoisoindolin-1-one
-
Human rhinovirus sp.
5-(bromoacetyl)-N-2-naphthylisophthalamide 5% inhibition at inhibitor concentration of 100 nM, 19% inhibition at inhibitor concentration of 1 microM, 80% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
5-(bromoacetyl)-N-phenylisophthalamide 8% inhibition at inhibitor concentration of 100 nM, 27% inhibition at inhibitor concentration of 1 microM, 86% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
5-(dibromoacetyl)-N-2-naphthylisophthalamide
-
Human rhinovirus sp.
5-(dibromoacetyl)-N-phenylisophthalamide
-
Human rhinovirus sp.
5-acetyl-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide
-
Human rhinovirus sp.
5-acetyl-N-phenylbenzene-1,3-dicarboxamide
-
Human rhinovirus sp.
6-(bromoacetyl)isoindolyn-1-one 0% inhibition at inhibitor concentration of 100 nM, 25% inhibition at inhibitor concentration of 1 microM, 70% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
6-acetylisoindolin1-one
-
Human rhinovirus sp.
6-bromoisoindolin-1-one
-
Human rhinovirus sp.
AG7088 inhibits all 48 serotypes of rhinoviruses Human rhinovirus sp.
AL21-01 Agouron aldehydic compound, 8% inhibition at inhibitor concentration of 100 nM, 75% inhibition at inhibitor concentration of 1 microM, 92% inhibition at inhibitor concentration of 0.01 mM, 700 nM enzyme Human rhinovirus sp.
dimethyl 5-acetylbenzene-1,3-dicarboxylate
-
Human rhinovirus sp.
ethyl 3-amino-5-[1-(hydroxyamino)ethyl]benzoate
-
Human rhinovirus sp.
methyl 3-benzamido-5-{2,2-difluoro-1-[(2-methoxyethoxy)methoxy]ethenyl}benzoate
-
Human rhinovirus sp.
methyl 3-benzyl-5-bromobenzoate
-
Human rhinovirus sp.
methyl 3-bromo-5-(5,8-dihydronaphthalen-2-ylmethyl)benzoate
-
Human rhinovirus sp.
methyl 3-bromo-5-{2,2-difluoro-1-[(2-methoxyethoxy)methoxy]ethenyl}benzoate
-
Human rhinovirus sp.
methyl-3-(benzylamino)-5-carbamoylbenzoate
-
Human rhinovirus sp.
methyl-3-amino-5-carbamoylbenzoate
-
Human rhinovirus sp.
methyl-3-carbamoyl-5-(dibenzylamino)benzoate
-
Human rhinovirus sp.
methyl-3-{2,2-difluoro-1-[(2-methoxyethoxy)methoxy]ethenyl}-5-{[(trifluoromethyl)sulfonyl]oxy}benzoate
-
Human rhinovirus sp.

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Thr-Gly-Leu-Phe-Gln-Gly-Pro + H2O Human rhinovirus sp.
-
Thr-Gly-Leu-Phe-Gln + Gly-Pro
-
?

Organism

Organism UniProt Comment Textmining
Human rhinovirus sp.
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Glu-Ala-Leu-Phe-Gln-4-nitroanilide + H2O
-
Human rhinovirus sp. Glu-Ala-Leu-Phe-Gln + 4-nitroaniline
-
?
Thr-Gly-Leu-Phe-Gln-Gly-Pro + H2O
-
Human rhinovirus sp. Thr-Gly-Leu-Phe-Gln + Gly-Pro
-
?

Synonyms

Synonyms Comment Organism
3CP
-
Human rhinovirus sp.
protease 3C
-
Human rhinovirus sp.

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Human rhinovirus sp.

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Human rhinovirus sp.