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Literature summary for 2.3.2.5 extracted from
- The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders (2018), J. Biol. Inorg. Chem., 23, 1219-1226 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3) | Homo sapiens |
| recombinant expression of His-tagged wild-type enzyme in Escherichia coli strain BL21(DE3) | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| purified recombinant His-tagged enzyme double mutant Y115E/Y117E in complex with inhibitor SEN177 and Zn2+, vapor diffusion technique, mixing an equal volume of protein sample and precipitant solution, X-ray diffraction structure determination and analysis at 1.72 A resolution, molecular replacement with the structure PDB ID 4YU9 as template, modeling | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| Y115E/Y117E | site-directed mutagenesis | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-Benzylimidazole | weak inhibition; weak inhibition | Homo sapiens |  |
| 1-vinylimidazole | weak inhibition; weak inhibition | Homo sapiens | |
| additional information | crystal structures of weak binding inhibitors of human QC isozymes, all share the imidazole ring as the Zn(II) binding moiety, overview; crystal structures of weak binding inhibitors of human QC isozymes, share the imidazole ring as the Zn(II) binding moiety, overview | Homo sapiens | |
| N-omega-acetylhistamine | weak inhibition; weak inhibition | Homo sapiens | |
| PBD150 | - |
Homo sapiens | |
| PQ912 | - |
Homo sapiens | |
| SEN177 | i.e. 6''-fluoro-4-(4-methyl-4H-[1,2,4]triazol-3-yl)-3,4,5,6-tetrahydro-2H-[1,2',3',3'']terpyridine, binding structure with Golgi-resident hQC; i.e. 6''-fluoro-4-(4-methyl-4H-[1,2,4]triazol-3-yl)-3,4,5,6-tetrahydro-2H-[1,2',3',3'']terpyridine, binding structure with secretory hQC | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | secretory isozyme | Homo sapiens | - |
- |
| Golgi apparatus | - |
Homo sapiens | 5794 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | required for catalysis | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-glutaminyl-peptide | Homo sapiens | - |
5-oxoprolyl-peptide + NH3 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q16769 | - |
- |
| Homo sapiens | Q9NXS2 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography | Homo sapiens |
| recombinant His-tagged wild-type enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| L-glutaminyl-peptide | - |
Homo sapiens | 5-oxoprolyl-peptide + NH3 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| glutaminyl cyclase | - |
Homo sapiens |
| Golgi resident glutaminyl cyclase | - |
Homo sapiens |
| gQC | - |
Homo sapiens |
| hQC | - |
Homo sapiens |
| secretory glutaminyl cyclase | - |
Homo sapiens |
| sQC | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 25 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 8 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
| 0.00002 | - |
SEN177 | pH 8.0, 25°C, with enzyme mutant Y115E/Y117E | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000247 | - |
pH 8.0, 25°C | Homo sapiens | PQ912 | |
| 0.00005 | - |
pH 8.0, 25°C, with enzyme mutant Y115E/Y117E | Homo sapiens | SEN177 | |
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