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Literature summary for 3.2.1.169 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)

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

Protein Variants

Protein Variants Comment Organism
V331C mutation of Val331 to cysteine results in a mutant enzyme with unaltered steady-state kinetics compared with wild-type CpOGA Clostridium perfringens
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

Inhibitors Comment Organism Structure
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
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
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
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
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
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
O-(2-acetamido-2-deoxy-D-glucopyranosylidene)amino N-phenylcarbamate PUGNAc Homo sapiens

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Clostridium perfringens Q0TR53
-
-
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Clostridium perfringens

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

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

Ki Value [mM]

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