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Literature summary for 2.4.1.65 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

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

Organism

Organism UniProt Comment Textmining
Helicobacter pylori
-
-
-
Homo sapiens
-
-
-

Synonyms

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

Ki Value [mM]

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

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