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Literature summary extracted from

  • Seelhorst, K.; Piernitzki, T.; Lunau, N.; Meier, C.; Hahn, U.
    Synthesis and analysis of potential alpha1,3-fucosyltransferase inhibitors (2014), Bioorg. Med. Chem., 22, 6430-6437.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.65 ADP about 30% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 dGDP about 40% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 dGDP about 76% inhibition at 0.4 mM Homo sapiens
2.4.1.65 GDP about 78% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 GDP about 80% inhibition at 0.4 mM Homo sapiens
2.4.1.65 GDP-6-amino-beta-L-fucose about 45% inhibition at 1 mM Helicobacter pylori
2.4.1.65 GDP-6-amino-beta-L-fucose 78% inhibition at 0.4 mM Homo sapiens
2.4.1.65 GTP about 70% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 GTP about 80% inhibition at 0.4 mM Homo sapiens
2.4.1.65 IDP about 60% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 IDP about 30% inhibition at 0.4 mM Homo sapiens
2.4.1.65 L-fucose about 20% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 additional information not inhibited by GMP Helicobacter pylori
2.4.1.65 additional information not inhibited by L-fucose, GMP and ADP Homo sapiens
2.4.1.65 [1-(beta-D-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate about 70% inhibition at 0.4 mM Homo sapiens
2.4.1.65 [1-(beta-D-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosinediphosphate about 74% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 [1-(beta-D-galactopyranosyl)-1H-1,2,3-triazole-4-yl] methylguanosine diphosphate about 76% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 [1-(beta-D-galactopyranosyl)-1H-1,2,3-triazole-4-yl] methylguanosine diphosphate about 73% inhibition at 0.4 mM Homo sapiens
2.4.1.65 [1-(beta-D-lactosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate about 60% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 [1-(beta-D-lactosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate about 45% inhibition at 0.4 mM Homo sapiens
2.4.1.65 [1-(beta-L-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate about 58% inhibition at 0.4 mM Helicobacter pylori
2.4.1.65 [1-(beta-L-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate about 60% inhibition at 0.4 mM Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.65 Helicobacter pylori
-
-
-
2.4.1.65 Homo sapiens
-
-
-

Synonyms

EC Number Synonyms Comment Organism
2.4.1.65 alpha1,3-fucosyltransferase
-
 Helicobacter pylori
2.4.1.65 alpha1,3-fucosyltransferase IX
-
 Homo sapiens
2.4.1.65 FucT
-
 Helicobacter pylori
2.4.1.65 FucT IX
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.65 0.0503
-
 dGDP at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.0779
-
 GDP at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.0807
-
 GTP at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.102
-
 GDP-6-amino-beta-L-fucose at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.137
-
 [1-(beta-L-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.186
-
 [1-(beta-D-galactopyranosyl)-1H-1,2,3-triazole-4-yl] methylguanosine diphosphate at pH 4.5 and 37°C Homo sapiens
2.4.1.65 0.19
-
 [1-(beta-D-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate at pH 4.5 and 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.65 0.049
-
 at pH 4.5 and 37°C Homo sapiens dGDP
2.4.1.65 0.059
-
 at pH 4.5 and 37°C Homo sapiens GDP
2.4.1.65 0.094
-
 at pH 4.5 and 37°C Homo sapiens GTP
2.4.1.65 0.104
-
 at pH 4.5 and 37°C Homo sapiens GDP-6-amino-beta-L-fucose
2.4.1.65 0.134
-
 at pH 4.5 and 37°C Homo sapiens [1-(beta-D-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate
2.4.1.65 0.139
-
 at pH 4.5 and 37°C Homo sapiens [1-(beta-L-fucopyranosyl)-1H-1,2,3-triazole-4-yl]methylguanosine diphosphate
2.4.1.65 0.247
-
 at pH 4.5 and 37°C Homo sapiens [1-(beta-D-galactopyranosyl)-1H-1,2,3-triazole-4-yl] methylguanosine diphosphate