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Literature summary for 2.3.2.5 extracted from

  • Schilling, S.; Niestroj, A.J.; Rahfeld, J.U.; Hoffmann, T.; Wermann, M.; Zunkel, K.; Wasternack, C.; Demuth, H.U.
    Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators (2003), J. Biol. Chem., 278, 49773-49779.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,10-phenanthroline inactivated enzyme can be fully restored by addition of Zn2+ in the presence of equimolar concentrations of EDTA, little reactivation by Co2+ and Mn2+ Homo sapiens
1,4-bis-(imidazol-1-yl)methyl-2,5-dimethylbenzene
-
Homo sapiens
1-(2-oxo-2-phenylethyl)-imidazole
-
Homo sapiens
1-(3-aminopropyl)-imidazole
-
Homo sapiens
1-(6-phenoxyhexyl)-1H-imidazole
-
Homo sapiens
1-Benzylimidazole
-
Homo sapiens
1-methyl-4-(beta-aminoethyl)-imidazole
-
Homo sapiens
1-methyl-5-(beta-aminoethyl)-imidazole
-
Homo sapiens
1-Methylimidazole
-
Homo sapiens
1-vinylimidazole
-
Homo sapiens
2-aminobenzimidazole
-
Homo sapiens
2-ethyl-4-methyl-imidazole
-
Homo sapiens
2-methyl-benzylimidazole
-
Homo sapiens
3-[3-(1H-imidazol-1-yl)propyl]-2-thioxoimidazolidin-4-one
-
Homo sapiens
4-(2-imidazol-1-yl-ethoxy)-benzoic acid
-
Homo sapiens
4-imidazole-carboxaldehyde
-
Homo sapiens
5-amino-3H-imidazole-4-carboxylic acid amide
-
Homo sapiens
5-hydroxymethyl-4-methyl-imidazole
-
Homo sapiens
benzimidazole
-
Homo sapiens
dipicolinic acid inactivated enzyme can be fully restored by addition of Zn2+ in the presence of equimolar concentrations of EDTA, little reactivation by Co2+ and Mn2+ Homo sapiens
H-His-Trp-OH
-
Homo sapiens
imidazol-4-carbonic acid methylester
-
Homo sapiens
imidazole
-
Homo sapiens
L-histamine
-
Homo sapiens
L-histidinamide
-
Homo sapiens
L-histidine
-
Homo sapiens
L-histidinol
-
Homo sapiens
N-(4-chlorophenyl)-N'-[2-(1H-imidazol-1-yl)propyl]-2-thioxoimidazolidin-4-one
-
Homo sapiens
N-(trimethylsilyl)-imidazole
-
Homo sapiens
N-Acetylimidazole
-
Homo sapiens
N-benzoylimidazole
-
Homo sapiens
N-omega-acetylhistamine
-
Homo sapiens
oxalic acid diimidazolidide
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Co2+ enzyme inactivated by 1,10-phenanthroline or dipicolinic acid can be restored partially by Co2+ or Mn2+ Homo sapiens
Mn2+ enzyme inactivated by 1,10-phenanthroline or dipicolinic acid can be restored partially by Co2+ or Mn2+ Homo sapiens
Zn2+ enzyme inactivated by 1,10-phenanthroline or dipicolinic acid can be fully restored by addition of Zn2+ in the presence of equimolar concentrations of EDTA Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16769
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gln-7-amido-4-methylcoumarin
-
Homo sapiens pyroglutamic acid-7-amido-4-methylcoumarin + NH3
-
?
Gln-Gln
-
Homo sapiens pyroglutamic acid-Gln + NH3
-
?

Synonyms

Synonyms Comment Organism
glutaminyl cyclase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0012
-
N-(4-chlorophenyl)-N'-[2-(1H-imidazol-1-yl)propyl]-2-thioxoimidazolidin-4-one 30°C, pH 8.0 Homo sapiens
0.0023
-
4-(2-imidazol-1-yl-ethoxy)-benzoic acid 30°C, pH 8.0 Homo sapiens
0.0062
-
1-(6-phenoxyhexyl)-1H-imidazole
-
Homo sapiens
0.0071
-
1-Benzylimidazole 30°C, pH 8.0 Homo sapiens
0.017
-
N-omega-acetylhistamine 30°C, pH 8.0 Homo sapiens
0.03
-
1-Methylimidazole 30°C, pH 8.0 Homo sapiens
0.049
-
1-vinylimidazole 30°C, pH 8.0 Homo sapiens
0.078
-
oxalic acid diimidazolidide 30°C, pH 8.0 Homo sapiens
0.103
-
imidazole 30°C, pH 8.0 Homo sapiens
0.107
-
N-Acetylimidazole 30°C, pH 8.0 Homo sapiens
0.12
-
1-methyl-5-(beta-aminoethyl)-imidazole 30°C, pH 8.0 Homo sapiens
0.129
-
5-hydroxymethyl-4-methyl-imidazole 30°C, pH 8.0 Homo sapiens
0.138
-
benzimidazole 30°C, pH 8.0 Homo sapiens
0.165
-
2-methyl-benzylimidazole 30°C, pH 8.0 Homo sapiens
0.167
-
N-(trimethylsilyl)-imidazole 30°C, pH 8.0 Homo sapiens
0.174
-
N-benzoylimidazole 30°C, pH 8.0 Homo sapiens
0.184
-
1-(2-oxo-2-phenylethyl)-imidazole 30°C, pH 8.0 Homo sapiens
0.295
-
1,4-bis-(imidazol-1-yl)methyl-2,5-dimethylbenzene 30°C, pH 8.0 Homo sapiens
0.41
-
1-(3-aminopropyl)-imidazole 30°C, pH 8.0 Homo sapiens
0.56
-
L-histidinamide 30°C, pH 8.0 Homo sapiens
0.58
-
2-ethyl-4-methyl-imidazole 30°C, pH 8.0 Homo sapiens
0.6
-
H-His-Trp-OH 30°C, pH 8.0 Homo sapiens
0.818
-
3-[3-(1H-imidazol-1-yl)propyl]-2-thioxoimidazolidin-4-one 30°C, pH 8.0 Homo sapiens
0.85
-
L-histamine 30°C, pH 8.0 Homo sapiens
1.53
-
L-histidinol 30°C, pH 8.0 Homo sapiens
1.8
-
2-aminobenzimidazole 30°C, pH 8.0 Homo sapiens
4.4
-
L-histidine 30°C, pH 8.0 Homo sapiens
7.6
-
4-imidazole-carboxaldehyde 30°C, pH 8.0 Homo sapiens
14.5
-
imidazol-4-carbonic acid methylester 30°C, pH 8.0 Homo sapiens
15.5
-
5-amino-3H-imidazole-4-carboxylic acid amide 30°C, pH 8.0 Homo sapiens