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Literature summary for 3.5.1.89 extracted from

  • Abdelwahab, N.Z.; Crossman, A.T.; Sullivan, L.; Ferguson, M.A.; Urbaniak, M.D.
    Inhibitors incorporating zinc-binding groups target the GlcNAc-PI de-N-acetylase in Trypanosoma brucei, the causative agent of African sleeping sickness (2012), Chem. Biol. Drug Des., 79, 270-278.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Trypanosoma brucei

Inhibitors

Inhibitors Comment Organism Structure
1,5-anhydro-2-(carboxymethyl)-2-deoxy-D-glucitol
-
Trypanosoma brucei
1,5-anhydro-2-deoxy-2-[2-(hydroxyamino)-2-oxoethyl]-D-glucitol
-
Trypanosoma brucei
1,5-anhydro-3-O-benzyl-2-(carboxymethyl)-2-deoxy-D-glucitol
-
Trypanosoma brucei
1,5-anhydro-3-O-benzyl-2-deoxy-2-[2-(hydroxyamino)-2-oxoethyl]-D-glucitol
-
Trypanosoma brucei
2-(carboxymethyl)-2-deoxy-D-glucopyranose
-
Trypanosoma brucei
phenyl 2-(carbamoylamino)-2-deoxy-1-thio-beta-D-glucopyranoside
-
Trypanosoma brucei
phenyl 2-(carboxymethyl)-2-deoxy-1-thio-alpha-D-glucopyranoside
-
Trypanosoma brucei
triethylammonium 1R,2R-1-O-[2-C-(carboxymethyl N-hydroxyamide)-2-deoxy-beta-D-glucopyranosyl]-cyclohexanediol 2-(n-octadecylphosphate)
-
Trypanosoma brucei

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ a zinc metalloenzyme Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
variant MITat1.4
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-GlcNAc-alpha(1->6)-D-myo-inositol-1-octadecyl phosphate + H2O
-
Trypanosoma brucei D-GlcN-alpha(1->6)-D-myo-inositol-1-octadecyl phosphate + acetate
-
?
N-acetyl-D-glucosaminylphosphatidylinositol + H2O + H2O
-
Trypanosoma brucei D-glucosaminylphosphatidylinositol + acetate
-
?

Synonyms

Synonyms Comment Organism
deNAc
-
Trypanosoma brucei
GlcNAc-PI de-N-acetylase
-
Trypanosoma brucei
N-acetylglucosamine-phosphatidylinositolde-N-acetylase
-
Trypanosoma brucei

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.019
-
in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei triethylammonium 1R,2R-1-O-[2-C-(carboxymethyl N-hydroxyamide)-2-deoxy-beta-D-glucopyranosyl]-cyclohexanediol 2-(n-octadecylphosphate)
0.1
-
in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei phenyl 2-(carboxymethyl)-2-deoxy-1-thio-alpha-D-glucopyranoside
0.29
-
in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei 1,5-anhydro-3-O-benzyl-2-(carboxymethyl)-2-deoxy-D-glucitol
0.3
-
in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei 2-(carboxymethyl)-2-deoxy-D-glucopyranose
1.5
-
in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei 1,5-anhydro-3-O-benzyl-2-deoxy-2-[2-(hydroxyamino)-2-oxoethyl]-D-glucitol
10
-
IC50 above 10 mM, in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei phenyl 2-(carboxymethyl)-2-deoxy-1-thio-alpha-D-glucopyranoside
10
-
IC50 above 10 mM, in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei 1,5-anhydro-2-(carboxymethyl)-2-deoxy-D-glucitol
10
-
IC50 above 10 mM, in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei 1,5-anhydro-2-deoxy-2-[2-(hydroxyamino)-2-oxoethyl]-D-glucitol
10
-
IC50 above 10 mM, in 50 mM Na-HEPES pH 7.4, 25 mM KCl, 0.1 mM Tos-LysCH2Cl and 0.001 mg/ml leupeptin, at 30°C Trypanosoma brucei phenyl 2-(carbamoylamino)-2-deoxy-1-thio-beta-D-glucopyranoside