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Literature summary for 3.2.1.169 extracted from

  • Borodkin, V.S.; Rafie, K.; Selvan, N.; Aristotelous, T.; Navratilova, I.; Ferenbach, A.T.; van Aalten, D.M.F.
    O-GlcNAcase fragment discovery with fluorescence polarimetry (2018), ACS Chem. Biol., 13, 1353-1360 .
    View publication on PubMed

Application

Application Comment Organism
medicine the enzyme is a drug target for the treatment of Alzheimer's and cardiovascular disease Homo sapiens
medicine the enzyme is a drug target for the treatment of Alzheimer's and cardiovascular disease Clostridium perfringens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3)-Gold cells Clostridium perfringens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop vapor diffusion method, using 0.175 M CdSO4 and 0.1 M sodium acetate at pH 7.5 Clostridium perfringens

Inhibitors

Inhibitors Comment Organism Structure
5-(trifluoromethyl)-2,3-dihydro-1H-1,4-diazepine
-
Clostridium perfringens
5-(trifluoromethyl)-2,3-dihydro-1H-1,4-diazepine
-
Homo sapiens
GlcNAcstatin B
-
Clostridium perfringens
GlcNAcstatin B
-
Homo sapiens
GlcNAcstatin BF
-
Clostridium perfringens
GlcNAcstatin BF
-
Homo sapiens
GlcNAcstatin C
-
Clostridium perfringens
GlcNAcstatin C
-
Homo sapiens
GlcNAcstatin G
-
Clostridium perfringens
GlcNAcstatin G
-
Homo sapiens
thiamet G
-
Clostridium perfringens
thiamet G
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-serine + H2O Homo sapiens
-
[protein]-L-serine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-serine + H2O Clostridium perfringens
-
[protein]-L-serine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-threonine + H2O Homo sapiens
-
[protein]-L-threonine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-threonine + H2O Clostridium perfringens
-
[protein]-L-threonine + N-acetyl-D-glucosamine
-
?

Organism

Organism UniProt Comment Textmining
Clostridium perfringens Q0TR53
-
-
Homo sapiens O60502
-
-

Purification (Commentary)

Purification (Comment) Organism
IMAC Sepharose column chromatography, Hi-Trap QFF column chromatography, and Superdex 200 gel filtration Clostridium perfringens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl beta-D-N-acetylglucosaminide + H2O
-
Homo sapiens 4-methylumbelliferone + beta-D-N-acetylglucosamine
-
?
4-methylumbelliferyl beta-D-N-acetylglucosaminide + H2O
-
Clostridium perfringens 4-methylumbelliferone + beta-D-N-acetylglucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-serine + H2O
-
Homo sapiens [protein]-L-serine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-serine + H2O
-
Clostridium perfringens [protein]-L-serine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-threonine + H2O
-
Homo sapiens [protein]-L-threonine + N-acetyl-D-glucosamine
-
?
[protein]-3-O-(N-acetyl-beta-D-glucosaminyl)-L-threonine + H2O
-
Clostridium perfringens [protein]-L-threonine + N-acetyl-D-glucosamine
-
?

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000163
-
GlcNAcstatin G pH and temperature not specified in the publication Clostridium perfringens
0.0000214
-
GlcNAcstatin G pH and temperature not specified in the publication Homo sapiens
0.0000232
-
GlcNAcstatin B pH and temperature not specified in the publication Homo sapiens
0.000037
-
thiamet G pH and temperature not specified in the publication Clostridium perfringens
0.000066
-
GlcNAcstatin B pH and temperature not specified in the publication Clostridium perfringens
0.0001531
-
thiamet G pH and temperature not specified in the publication Homo sapiens
0.146
-
5-(trifluoromethyl)-2,3-dihydro-1H-1,4-diazepine pH and temperature not specified in the publication Clostridium perfringens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000145
-
pH and temperature not specified in the publication Clostridium perfringens GlcNAcstatin B
0.0000429
-
pH and temperature not specified in the publication Clostridium perfringens GlcNAcstatin G
0.0000578
-
pH and temperature not specified in the publication Homo sapiens GlcNAcstatin G
0.0000626
-
pH and temperature not specified in the publication Clostridium perfringens thiamet G
0.0000632
-
pH and temperature not specified in the publication Homo sapiens GlcNAcstatin B
0.0001501
-
pH and temperature not specified in the publication Homo sapiens thiamet G