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Literature summary for 3.2.1.18 extracted from

  • Tu, V.; Abed, Y.; Fage, C.; Baz, M.; Boivin, G.
    Impact of R152K and R368K neuraminidase catalytic substitutions on in vitro properties and virulence of recombinant A(H1N1)pdm09 viruses (2018), Antiviral Res., 154, 110-115 .
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
R152K the mutation mediates reduced inhibition by oseltamivir, zanamivir, peramivir and laninamivir (10-100fold increase of IC50 value compared to the wild type enzyme) unidentified influenza virus
R152K/V94I the mutations mediate reduced inhibition by oseltamivir, zanamivir, peramivir and laninamivir (10-100fold increase of IC50 value compared to the wild type enzyme) unidentified influenza virus
R368K the mutation mediates reduced inhibition by oseltamivir, zanamivir and laninamivir (96-57fold increase of IC50 value compared to the wild type enzyme) as well as peramivir (172fold increase of IC50 value compared to the wild type enzyme) unidentified influenza virus
V94IK the mutant shows normal inhibition by oseltamivir, zanamivir, peramivir and laninamivir unidentified influenza virus

Inhibitors

Inhibitors Comment Organism Structure
2,3-dehydro-2-deoxy-N-acetylneuraminic acid weak inhibitor unidentified influenza virus
laninamivir
-
unidentified influenza virus
oseltamivir
-
unidentified influenza virus
peramivir
-
unidentified influenza virus
zanamivir
-
unidentified influenza virus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.01506
-
4-methylumbelliferyl N-acetylneuraminic acid mutant enzyme V94I, at 37°C, pH not specified in the publication unidentified influenza virus
0.02
-
4-methylumbelliferyl N-acetylneuraminic acid wild type enzyme, at 37°C, pH not specified in the publication unidentified influenza virus
0.2008
-
4-methylumbelliferyl N-acetylneuraminic acid mutant enzyme R368K, at 37°C, pH not specified in the publication unidentified influenza virus
0.2355
-
4-methylumbelliferyl N-acetylneuraminic acid mutant enzyme R152K/V94I, at 37°C, pH not specified in the publication unidentified influenza virus
0.5652
-
4-methylumbelliferyl N-acetylneuraminic acid mutant enzyme R152K, at 37°C, pH not specified in the publication unidentified influenza virus

Organism

Organism UniProt Comment Textmining
unidentified influenza virus
-
-
-
unidentified influenza virus A/Quebec/144147/09
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl N-acetylneuraminic acid + H2O
-
unidentified influenza virus 4-methylumbelliferone + N-acetylneuraminic acid
-
?
4-methylumbelliferyl N-acetylneuraminic acid + H2O
-
unidentified influenza virus A/Quebec/144147/09 4-methylumbelliferone + N-acetylneuraminic acid
-
?

Synonyms

Synonyms Comment Organism
neuraminidase
-
unidentified influenza virus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00016
-
mutant enzyme V94I, at 37°C, pH not specified in the publication unidentified influenza virus peramivir
0.0002
-
wild type enzyme, at 37°C, pH not specified in the publication unidentified influenza virus peramivir
0.00036
-
wild type enzyme, at 37°C, pH not specified in the publication unidentified influenza virus laninamivir
0.00066
-
mutant enzyme V94I, at 37°C, pH not specified in the publication unidentified influenza virus zanamivir
0.00068
-
wild type enzyme, at 37°C, pH not specified in the publication unidentified influenza virus zanamivir
0.0009
-
mutant enzyme V94I, at 37°C, pH not specified in the publication unidentified influenza virus laninamivir
0.00142
-
mutant enzyme V94I, at 37°C, pH not specified in the publication unidentified influenza virus oseltamivir
0.00148
-
wild type enzyme, at 37°C, pH not specified in the publication unidentified influenza virus oseltamivir
0.00181
-
mutant enzyme R152K, at 37°C, pH not specified in the publication unidentified influenza virus laninamivir
0.00649
-
mutant enzyme R152K/V94I, at 37°C, pH not specified in the publication unidentified influenza virus laninamivir
0.00804
-
mutant enzyme R368K, at 37°C, pH not specified in the publication unidentified influenza virus laninamivir
0.0114
-
mutant enzyme R152K/V94I, at 37°C, pH not specified in the publication unidentified influenza virus peramivir
0.0148
-
mutant enzyme R368K, at 37°C, pH not specified in the publication unidentified influenza virus peramivir
0.01768
-
mutant enzyme R368K, at 37°C, pH not specified in the publication unidentified influenza virus zanamivir
0.01776
-
mutant enzyme R152K/V94I, at 37°C, pH not specified in the publication unidentified influenza virus zanamivir
0.0344
-
mutant enzyme R152K, at 37°C, pH not specified in the publication unidentified influenza virus peramivir
0.03936
-
mutant enzyme R152K, at 37°C, pH not specified in the publication unidentified influenza virus zanamivir
0.07812
-
mutant enzyme R152K/V94I, at 37°C, pH not specified in the publication unidentified influenza virus oseltamivir
0.10048
-
mutant enzyme R368K, at 37°C, pH not specified in the publication unidentified influenza virus oseltamivir
0.14252
-
mutant enzyme R152K, at 37°C, pH not specified in the publication unidentified influenza virus oseltamivir