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Literature summary extracted from

  • Dorfmueller, H.C.; Borodkin, V.S.; Schimpl, M.; van Aalten, D.M.F.
    GlcNAcstatins are nanomolar inhibitors of human O-GlcNAcase inducing cellular hyper-O-GlcNAcylation (2009), Biochem. J., 420, 221-227.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.2.1.169
-
 Clostridium perfringens
3.2.1.169 expressed in Escherichia coli BL21 Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.2.1.169 V331C mutation of Val331 to cysteine results in a mutant enzyme with unaltered steady-state kinetics compared with wild-type CpOGA Clostridium perfringens
3.2.1.169 W490A mutation of Trp490 to alanine results in a mutant enzyme that shows a 30fold reduction in Km when assayed with the pseudosubstrate 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide Clostridium perfringens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.169 GlcNAcstatin A GlcNAcstatin A carries a carboxymethyl group, GlcNAcstatins are the most potent human O-GlcNAcase inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Homo sapiens
3.2.1.169 GlcNAcstatin B GlcNAcstatin B carries a phenylethyl moiety. GlcNAcstatins are the most potent human O-GlcNAcase inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Homo sapiens
3.2.1.169 GlcNAcstatin C GlcNAcstatin C carriesa phenylethyl moiety. GlcNAcstatins are the most potent human OGA inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Clostridium perfringens
3.2.1.169 GlcNAcstatin C GlcNAcstatin C carriesa phenylethyl moiety. GlcNAcstatins are the most potent human O-GlcNAcase inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Homo sapiens
3.2.1.169 GlcNAcstatin D GlcNAcstatin D carries a phenylethyl moiety. GlcNAcstatins are the most potent human O-GlcNAcase inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Homo sapiens
3.2.1.169 GlcNAcstatin E GlcNAcstatin E carries a phenylethyl moiety. GlcNAcstatins are the most potent human O-GlcNAcase inhibitors, inhibiting the enzyme in the sub-nanomolar to nanomolar range Homo sapiens
3.2.1.169 O-(2-acetamido-2-deoxy-D-glucopyranosylidene)amino N-phenylcarbamate PUGNAc Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.2.1.169 0.0029
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide wild-type Clostridium perfringens
3.2.1.169 0.0068
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide V331C mutant Clostridium perfringens
3.2.1.169 0.1
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide W490A mutant Clostridium perfringens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.2.1.169 additional information Homo sapiens enzyme that removes N-acetyl-beta-D-glucosamine from O-GlcNAcylated proteins ?
-
 ?
3.2.1.169 additional information Clostridium perfringens enzyme that removes O-GlcNAc from O-GlcNAcylated proteins ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.2.1.169 Clostridium perfringens Q0TR53
-
-
3.2.1.169 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.2.1.169
-
 Clostridium perfringens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.2.1.169 HEK-293 cell
-
 Homo sapiens
-
3.2.1.169 HeLa cell
-
 Homo sapiens
-
3.2.1.169 HT-1080 cell
-
 Homo sapiens
-
3.2.1.169 SH-SY5Y cell
-
 Homo sapiens
-
3.2.1.169 U2-OS cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.169 4-methylumbelliferyl N-acetyl-beta-D-glucosaminide + H2O fluorogenic substrate, 4MU-NAG Homo sapiens 4-methylumbelliferone + N-acetyl-beta-D-glucosamine
-
 ?
3.2.1.169 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide + H2O fluorogenic substrate, 4MU-NAG Clostridium perfringens 4-methylumbelliferone + N-acetyl-beta-D-glucosamine
-
 ?
3.2.1.169 additional information enzyme that removes N-acetyl-beta-D-glucosamine from O-GlcNAcylated proteins Homo sapiens ?
-
 ?
3.2.1.169 additional information enzyme that removes O-GlcNAc from O-GlcNAcylated proteins Clostridium perfringens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.1.169 CpOGA
-
 Clostridium perfringens
3.2.1.169 hOGA
-
 Homo sapiens
3.2.1.169 O-GlcNAcase
-
 Homo sapiens
3.2.1.169 O-GlcNAcase
-
 Clostridium perfringens
3.2.1.169 OGA
-
 Homo sapiens
3.2.1.169 OGA
-
 Clostridium perfringens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.2.1.169 10.5
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide wild-type Clostridium perfringens
3.2.1.169 17.3
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide V331C mutant Clostridium perfringens
3.2.1.169 65
-
 4-methylumbelliferyl-N-acetyl-beta-D-glucosaminide W490A mutant Clostridium perfringens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.2.1.169 0.00000042
-
 GlcNAcstatin B
-
 Homo sapiens
3.2.1.169 0.00000074
-
 GlcNAcstatin D
-
 Homo sapiens
3.2.1.169 0.0000043
-
 GlcNAcstatin A
-
 Homo sapiens
3.2.1.169 0.0000044
-
 GlcNAcstatin C
-
 Homo sapiens
3.2.1.169 0.0000046
-
 GlcNAcstatin C wild-type Clostridium perfringens
3.2.1.169 0.000035
-
 O-(2-acetamido-2-deoxy-D-glucopyranosylidene)amino N-phenylcarbamate
-
 Homo sapiens
3.2.1.169 0.000074
-
 GlcNAcstatin C W490A mutant Clostridium perfringens
3.2.1.169 0.0000981
-
 GlcNAcstatin C V331C mutant Clostridium perfringens
3.2.1.169 0.0085
-
 GlcNAcstatin E
-
 Homo sapiens