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Literature summary for 3.2.1.18 extracted from

  • Pokorna, J.; Pachl, P.; Karlukova, E.; Hejdanek, J.; Rezacova, P.; Machara, A.; Hudlicky, J.; Konvalinka, J.; Kozisek, M.
    Kinetic, Thermodynamic, and structural analysis of drug resistance mutations in neuraminidase from the 2009 pandemic Influenza virus (2018), Viruses, 10, E339 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.2.1.18

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Drosophila melanogaster Schneider S2 cells influenza A virus H1N1

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant enzymes in complex with oseltamivir carboxylate, hanging drop vapor diffusion method, mutant I223V: 0.1 M HEPES pH 6.75, 7% (w/v) PEG 8000, mutant S247N: 0.1 M HEPES pH 6.7, 8.5% (w/v) PEG 8000, mutant H275Y: 0.1 M HEPES pH 7.0, 8% (w/v) PEG 8000, mutant I223V/H275Y: 0.1 M HEPES pH 7.0, 7% (w/v) PEG 8000, and mutant S247N/H275Y: 0.1 M HEPES pH 7.5, 5% (w/v) PEG 8000 influenza A virus H1N1

Protein Variants

Protein Variants Comment Organism
H275Y the major oseltamivir resistance mutation H275Y causes a significant decrease in the enzyme's ability to bind oseltamivir influenza A virus H1N1
H275Y/I223V the mutations result in extreme impairment of oseltamivir's inhibition potency influenza A virus H1N1
H275Y/S247N the mutations result in extreme impairment of oseltamivir's inhibition potency influenza A virus H1N1
I223V the substitution alone confers only a moderate reduction in oseltamivir affinity influenza A virus H1N1
S247N the substitution alone confers only a moderate reduction in oseltamivir affinity influenza A virus H1N1

Inhibitors

Inhibitors Comment Organism Structure
oseltamivir
-
 influenza A virus H1N1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid wild type enzyme, at 37°C, pH not specified in the publication influenza A virus H1N1
1.1
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y, at 37°C, pH not specified in the publication influenza A virus H1N1
1.1
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
1.2
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
1.3
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
3.3
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/S247N, at 37°C, pH not specified in the publication influenza A virus H1N1

Organism

Organism UniProt Comment Textmining
influenza A virus H1N1 C3W6G3 A/California/07/2009
-

Purification (Commentary)

Purification (Comment) Organism
Strep-Tactin resin column chromatography influenza A virus H1N1

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl alpha-D-N-acetylneuraminic acid + H2O
-
 influenza A virus H1N1 4-methylumbelliferone + alpha-D-N-acetylneuraminic acid
-
 ?

Synonyms

Synonyms Comment Organism
neuraminidase
-
 influenza A virus H1N1

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.045
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.054
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y, at 37°C, pH not specified in the publication influenza A virus H1N1
0.1
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
0.17
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
0.6
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.9
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid wild type enzyme, at 37°C, pH not specified in the publication influenza A virus H1N1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000024
-
 oseltamivir wild type enzyme, at 37°C, pH not specified in the publication influenza A virus H1N1
0.00045
-
 oseltamivir mutant enzyme S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
0.0007
-
 oseltamivir mutant enzyme I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.027
-
 oseltamivir mutant enzyme H275Y, at 37°C, pH not specified in the publication influenza A virus H1N1
0.094
-
 oseltamivir mutant enzyme H275Y/I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.22
-
 oseltamivir mutant enzyme H275Y/S247N, at 37°C, pH not specified in the publication influenza A virus H1N1

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.031
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
0.035
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y/I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.048
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme H275Y, at 37°C, pH not specified in the publication influenza A virus H1N1
0.16
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme S247N, at 37°C, pH not specified in the publication influenza A virus H1N1
0.51
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid mutant enzyme I223V, at 37°C, pH not specified in the publication influenza A virus H1N1
0.82
-
 4-methylumbelliferyl alpha-D-N-acetylneuraminic acid wild type enzyme, at 37°C, pH not specified in the publication influenza A virus H1N1