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Literature summary for 2.4.1.255 extracted from

  • Dorfmueller, H.C.; Borodkin, V.S.; Blair, D.E.; Pathak, S.; Navratilova, I.; van Aalten, D.M.
    Substrate and product analogues as human O-GlcNAc transferase inhibitors (2011), Amino Acids, 40, 781-972.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.1.255

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
vapour diffusion crystallisation experiments are performed Homo sapiens

Protein Variants

Protein Variants Comment Organism
hOGT (26-end) mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5'-O-[hydroxy(phosphonomethyl)phosphoryl]uridine non-hydrolysable alpha,beta-methylene bisphosphonate analogue with the diphosphate oxygen replaced by a methylene group Homo sapiens
alloxan low micromolar inhibitor Homo sapiens
additional information testing UDP-GlcNAc/UDP analogues and evaluate their inhibitory properties and structural binding modes in vitro. These analogues are not active on living cells, they inhibit the enzyme in the micromolar range and together with the structural data provide useful templates for further optimisation Homo sapiens
UDP product inhibition Homo sapiens
UDP-1-deoxy-1-methylene-N-acetyl-alpha-D-glucosamine weak hOGT inhibitor Homo sapiens
UDP-1-deoxy-1-thio-N-acetyl-alpha-D-glucosamine a sub-millimolar inhibitor of hOGT and substrate binding probe Homo sapiens
UDP-S-GlcNAc
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information kinetic experiments using recombinant hOGT/XcOGT Homo sapiens
0.001
-
 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 GlcNAc onto substrate proteins using UDP-GlcNAc as the sugar donor ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme transfers GlcNAc onto substrate proteins using UDP-GlcNAc as the sugar donor Homo sapiens ?
-
 ?
additional information UDP-1-deoxy-1-thio-N-acetyl-alpha-D-glucosamine is no substrate Homo sapiens ?
-
 ?
YSDSPSTST + UDP-GlcNAc
-
 Homo sapiens UDP + ?
-
 ?

Synonyms

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

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
additional information
-
 hOGT assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0018
-
-
 Homo sapiens UDP
0.009
-
-
 Homo sapiens 5'-O-[hydroxy(phosphonomethyl)phosphoryl]uridine
0.018
-
-
 Homo sapiens alloxan
0.041
-
-
 Homo sapiens UDP-1-deoxy-1-methylene-N-acetyl-alpha-D-glucosamine
0.093
-
-
 Homo sapiens UDP-1-deoxy-1-thio-N-acetyl-alpha-D-glucosamine