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Literature summary for 2.4.1.255 extracted from

  • Trapannone, R.; Rafie, K.; van Aalten, D.M.
    O-GlcNAc transferase inhibitors current tools and future challenges (2016), Biochem. Soc. Trans., 44, 88-93 .
    View publication on PubMed
Search for more literature for 2.4.1.255

Inhibitors

Inhibitors Comment Organism Structure
2,4,5,6-tetraoxypyrimidine
-
 Homo sapiens
3-(2-adamantanylethyl)-2-[(4-chlorophenyl)azamethylene]-4-oxo-1,3-thiazaperhydroine-6-carboxylic acid
-
 Homo sapiens
4-methoxyphenyl 6-acetyl-2-oxobenzo[d]oxazole-3(2H)-carboxylate
-
 Homo sapiens
benzyl-2-acetamido-2-deoxy-alpha-D-galactopyranoside
-
 Homo sapiens
C-UDP
-
 Homo sapiens
UDP
-
 Homo sapiens
UDP-5-thio-N-acetyl-alpha-D-glucosamine
-
 Homo sapiens
UDP-C-GlcNAc
-
 Homo sapiens
UDP-S-GlcNAc
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O15294
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac4-5S-GlcNAc + [protein]-L-serine the donor substrate analogues Ac4-5S-GlcNAc and benzyl-2-acetamido-2-deoxy-alpha-D-galactopyranoside, might reduce the flux through the hexosamine pathway and reduce the amount of intracellular UDP-GlcNAc with potential side effects on glycan synthesis Homo sapiens UDP + ?
-
 ?
benzyl-2-acetamido-2-deoxy-alpha-D-galactopyranoside + [protein]-L-serine the donor substrate analogues Ac4-5S-GlcNAc and benzyl-2-acetamido-2-deoxy-alpha-D-galactopyranoside, might reduce the flux through the hexosamine pathway and reduce the amount of intracellular UDP-GlcNAc with potential side effects on glycan synthesis Homo sapiens UDP + ?
-
 ?

Synonyms

Synonyms Comment Organism
O-GlcNAc transferase
-
 Homo sapiens
OGT
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0018
-
 pH and temperature not specified in the publication Homo sapiens UDP
0.009
-
 pH and temperature not specified in the publication Homo sapiens C-UDP
0.01
-
 pH and temperature not specified in the publication Homo sapiens 4-methoxyphenyl 6-acetyl-2-oxobenzo[d]oxazole-3(2H)-carboxylate
0.018
-
 pH and temperature not specified in the publication Homo sapiens 2,4,5,6-tetraoxypyrimidine
0.041
-
 pH and temperature not specified in the publication Homo sapiens UDP-C-GlcNAc
0.053
-
 pH and temperature not specified in the publication Homo sapiens 3-(2-adamantanylethyl)-2-[(4-chlorophenyl)azamethylene]-4-oxo-1,3-thiazaperhydroine-6-carboxylic acid
0.093
-
 pH and temperature not specified in the publication Homo sapiens UDP-S-GlcNAc

General Information

General Information Comment Organism
malfunction O-GlcNAc transferase knockout is embryonic lethal in a range of animal models Homo sapiens
physiological function O-GlcNAc modification is abundant, essential and involved in fundamental biological processes Homo sapiens