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Literature summary for 3.2.1.18 extracted from

  • Li, Y.; Cao, H.; Yu, H.; Chen, Y.; Lau, K.; Qu, J.; Thon, V.; Sugiarto, G.; Chen, X.
    Identifying selective inhibitors against the human cytosolic sialidase NEU2 by substrate specificity studies (2011), Mol. Biosyst., 7, 1060-1072.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
isozyme NEU2, DNA and amino acid sequence determination and analysis, overexpression as soluble active enzyme in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,6-anhydro-3,5-dideoxy-5-glycolylamido-D-glycero-D-galactonon-2-enonic acid
-
Homo sapiens
2,6-anhydro-3-deoxy-D-glycero-D-galacto-non-2-enonic acid
-
Homo sapiens
2,6-anhydro-5-(2-azidoacetamido)-3,5-dideoxy-D-glycero-D-galacto-non-2-enonic acid
-
Homo sapiens
5-acetamido-2,6-anhydro-3,5-dideoxy-D-glycero-D-galactonon-2-enonic acid
-
Homo sapiens
Ca2+
-
Homo sapiens
Co2+
-
Homo sapiens
Cu2+ 95% inhibition at 10 mM Homo sapiens
EDTA 20% inhibition at 1 mM, 54% at 10 mM Homo sapiens
Li+ 9% inhibition at 10 mM Homo sapiens
Mg2+
-
Homo sapiens
Mn2+ 28% inhibition at 10 mM Homo sapiens
additional information design of a sialidase inhibitor selective against human NEU2, inhibitor docking using also the crystal structure of the enzyme, overview Homo sapiens
zanamivir
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme NEU2
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein one potential N-linked glycosylation site Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(N-glycolylneuraminic acid)(alpha2,3)Galbeta-p-nitrophenol + H2O
-
Homo sapiens N-glycolylneuraminic acid + 4-nitrophenol + ?
-
?
(N-glycolylneuraminic acid)(alpha2,6)Galbeta-p-nitrophenol + H2O
-
Homo sapiens N-glycolylneuraminic acid + 4-nitrophenol + ?
-
?
2'-(4-methyl-umbelliferyl) alpha-D-N-acetylneuraminic acid + H2O
-
Homo sapiens 4-methyl-umbelliferol + alpha-D-N-acetylneuraminic acid
-
?
5-acetylneuraminic acid-(alpha2,3)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-acetylneuraminic acid + 4-nitrophenol + ?
-
?
5-acetylneuraminic acid-(alpha2,6)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-acetylneuraminic acid + 4-nitrophenol + ?
-
?
5-azidoacetylneuraminic acid-(alpha2,3)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-azidoacetylneuraminic acid + 4-nitrophenol + ?
-
?
5-azidoacetylneuraminic acid-(alpha2,6)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-azidoacetylneuraminic acid + 4-nitrophenol + ?
-
?
5-fluoroacetylneuraminic acid-(alpha2,3)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-fluoroacetylneuraminic acid + 4-nitrophenol + ?
-
?
5-fluoroacetylneuraminic acid-(alpha2,6)Galbeta-4-nitrophenol + H2O
-
Homo sapiens N-fluoroacetylneuraminic acid + 4-nitrophenol + ?
-
?
additional information both alpha2-3- and alpha2-6-linked sialosides are suitable substrates for NEU2 although it cleaves alpha2-3-linked sialosides more efficiently. Twenty 4-nitrophenyl-tagged alpha(2,3)- or alpha(2,6)-linked sialyl galactosides containing different terminal sialic acid forms including common N-acetylneuraminic acid, non-human N-glycolylneuraminic acid, 2-keto-3-deoxy-D-glycero-D-galacto-nonulosonic acid, or their C5-derivatives are used as substrates, overview Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
NEU2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5
-
-
Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
4.5 6.5 activity range, almost inactive at pH 4.0 and pH 7.0 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0053
-
pH 5.5, 37°C Homo sapiens zanamivir
0.0083
-
pH 5.5, 37°C Homo sapiens 2,6-anhydro-5-(2-azidoacetamido)-3,5-dideoxy-D-glycero-D-galacto-non-2-enonic acid
0.018
-
pH 5.5, 37°C Homo sapiens 5-acetamido-2,6-anhydro-3,5-dideoxy-D-glycero-D-galactonon-2-enonic acid
0.034
-
pH 5.5, 37°C Homo sapiens 2,6-anhydro-3,5-dideoxy-5-glycolylamido-D-glycero-D-galactonon-2-enonic acid
2.1
-
pH 5.5, 37°C Homo sapiens 2,6-anhydro-3-deoxy-D-glycero-D-galacto-non-2-enonic acid