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Literature summary for 2.4.1.255 extracted from

  • Gross, B.J.; Kraybill, B.C.; Walker, S.
    Discovery of O-GlcNAc transferase inhibitors (2005), J. Am. Chem. Soc., 127, 14588-14589.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
ncOGT, mOGT, and sOGT constructs are cloned into a modified pET-24b vector for expression as C-terminal His8 fusions. Expression in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-[(4-chlorophenyl)imino]-4-oxo-3-(2-tricyclo[3.3.1.1(3,7)]dec-1-ylethyl)-1,3-thiazinane-6-carboxylic acid donor analogue displacement probes Homo sapiens
3-(4-cyanobenzylthio)-1-(thiophen-2-yl)-5,6,7,8-tetrahydroisoquinoline-4-carboxylic acid donor analogue displacement probes Homo sapiens
phenyl 6-chloro-2-oxobenzo[d]oxazole-3(2H)-carboxylate donor analogue displacement probes Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0067
-
UDP-GlcNAc
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme transfers N-acetylglucosamine from UDP-GlcNAc to selected serine and threonine residues ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.161
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme transfers N-acetylglucosamine from UDP-GlcNAc to selected serine and threonine residues Homo sapiens ?
-
?
UDP-GlcNAc + Nup62 protein
-
Homo sapiens UDP + N-acetyl-D-glucosmainyl-[Nup62 protein]
-
?

Subunits

Subunits Comment Organism
More OGT is a bipartite protein consisting of a C-terminal glycosyltransferase (Gtf) domain and an N-terminal protein-protein interaction domain comprised of 12 tetratricopeptide (TPR) repeats Homo sapiens

Synonyms

Synonyms Comment Organism
mOGT splice variant Homo sapiens
ncOGT splice variant Homo sapiens
O-GlcNAc transferase
-
Homo sapiens
OGT
-
Homo sapiens
sOGT splice variant Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
for ncOGT IC50 value is about 100-150 microM Homo sapiens 3-(4-cyanobenzylthio)-1-(thiophen-2-yl)-5,6,7,8-tetrahydroisoquinoline-4-carboxylic acid
0.01
-
ncOGT Homo sapiens phenyl 6-chloro-2-oxobenzo[d]oxazole-3(2H)-carboxylate
0.027
-
sOGT Homo sapiens phenyl 6-chloro-2-oxobenzo[d]oxazole-3(2H)-carboxylate
0.03
-
sOGT Homo sapiens (2Z)-2-[(4-chlorophenyl)imino]-4-oxo-3-(2-tricyclo[3.3.1.1(3,7)]dec-1-ylethyl)-1,3-thiazinane-6-carboxylic acid
0.053
-
ncOGT Homo sapiens (2Z)-2-[(4-chlorophenyl)imino]-4-oxo-3-(2-tricyclo[3.3.1.1(3,7)]dec-1-ylethyl)-1,3-thiazinane-6-carboxylic acid
0.06
-
sOGT Homo sapiens 3-(4-cyanobenzylthio)-1-(thiophen-2-yl)-5,6,7,8-tetrahydroisoquinoline-4-carboxylic acid

General Information

General Information Comment Organism
metabolism O-GlcN acylation affects such diverse cellular processes as transcription, translation, organelle targeting, and protein-protein interactions,1 and is believed to play a role in a variety of signaling cascades that mediate glucose homeostasis and stress responses Homo sapiens