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Literature summary extracted from

  • Magesh, S.; Savita, V.; Moriya, S.; Suzuki, T.; Miyagi, T.; Ishida, H.; Kiso, M.
    Human sialidase inhibitors: design, synthesis, and biological evaluation of 4-acetamido-5-acylamido-2-fluoro benzoic acids (2009), Bioorg. Med. Chem., 17, 4595-4603.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.18 2-deoxy-2,3-dehydro-N-acetylneuraminic acid
-
 Homo sapiens
3.2.1.18 4,5-diacetamido-2-fluorobenzoate 8% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 4,5-diacetamido-2-fluorobenzoic acid 23% inhibition of isoform NEU3 at 1 mM; 37% inhibition of isoform NEU2 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-(2-ethylbutanamido)-2-fluorobenzoic acid 23% inhibition of isoform NEU2 at 1 mM; less than 5% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-(2-methylbutanamido)-2-fluorobenzoic acid 7% inhibition of isoform NEU2 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-(2-naphthamido)-2-fluorobenzoic acid 10% inhibition of isoform NEU4 at 1 mM; 33% inhibition of isoform NEU2 at 1 mM; 8% inhibition of isoform NEU3 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-(biphenyl-4-ylcarboxamido)-2-fluorobenzoic acid 10% inhibition of isoform NEU4 at 1 mM; 60% inhibition of isoform NEU2 at 1 mM; 8% inhibition of isoform NEU3 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-benzamido-2-fluorobenzoic acid 17% inhibition of isoform NEU2 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-cyclohexanecarboxamido-2-fluorobenzoic acid 17% inhibition of isoform NEU2 at 1 mM; 6% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-cyclopropanecarboxamido-2-fluorobenzoic acid 20% inhibition of isoform NEU2 at 1 mM; less than 5% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-isobutyramido-2-fluorobenzoic acid 11% inhibition of isoform NEU4 at 1 mM; 15% inhibition of isoform NEU2 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-pentanamido-2-fluorobenzoic acid 13% inhibition of isoform NEU3 at 1 mM; 25% inhibition of isoform NEU2 at 1 mM; less than 5% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 4-acetamido-5-pivalamido-2-fluorobenzoic acid less than 5% inhibition of isoform NEU4 at 1 mM Homo sapiens
3.2.1.18 additional information no inhibition by 4-acetamido-5-cyclopentanecarboxamido-2-fluoro benzoic acid of isoform NEU1 at 1 mM; no inhibition by 4-acetamido-5-cyclopentanecarboxamido-2-fluoro benzoic acid of NEU2 isoform at 1 mM; no inhibition by 4-acetamido-5-cyclopentanecarboxamido-2-fluoro benzoic acid of NEU3 isoform at 1 mM; no inhibition by 4-acetamido-5-cyclopentanecarboxamido-2-fluoro benzoic acid of NEU4 isoform at 1 mM Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.2.1.18 cytosol isoform NEU2 Homo sapiens 5829
-
3.2.1.18 lysosome
-
 Homo sapiens 5764
-
3.2.1.18 mitochondrion
-
 Homo sapiens 5739
-
3.2.1.18 plasma membrane isoform NEU3 Homo sapiens 5886
-

Organism

EC Number Organism UniProt Comment Textmining
3.2.1.18 Homo sapiens Q8WWR8
-
-
3.2.1.18 Homo sapiens Q99519
-
-
3.2.1.18 Homo sapiens Q9UQ49
-
-
3.2.1.18 Homo sapiens Q9Y3R4
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.18 4-methylumbelliferyl-alpha-D-N-acetylneuraminic acid + H2O
-
 Homo sapiens 4-methylumbelliferone + N-acetylneuraminic acid
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.1.18 alpha-N-acylneuraminate glycohydrolase
-
 Homo sapiens
3.2.1.18 exo-alpha-sialidase
-
 Homo sapiens
3.2.1.18 NEU1 isoform Homo sapiens
3.2.1.18 NEU2 isoform Homo sapiens
3.2.1.18 Neu3 isoform Homo sapiens
3.2.1.18 NEU4 isoform Homo sapiens
3.2.1.18 neuramindase
-
 Homo sapiens
3.2.1.18 sialidase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.2.1.18 0.552
-
 isoform NEU2 Homo sapiens 4-acetamido-5-(biphenyl-4-ylcarboxamido)-2-fluorobenzoic acid
3.2.1.18 5
-
 IC50 above 5 mM, isoform NEU3 Homo sapiens 4-acetamido-5-(biphenyl-4-ylcarboxamido)-2-fluorobenzoic acid
3.2.1.18 5
-
 IC50 above 5 mM, isoform NEU4 Homo sapiens 4-acetamido-5-(biphenyl-4-ylcarboxamido)-2-fluorobenzoic acid