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Literature summary extracted from

  • Pozzi, C.; Di Pisa, F.; Benvenuti, M.; Mangani, S.
    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 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.2.5 recombinant expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3) Homo sapiens
2.3.2.5 recombinant expression of His-tagged wild-type enzyme in Escherichia coli strain BL21(DE3) Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.3.2.5 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

EC Number Protein Variants Comment Organism
2.3.2.5 Y115E/Y117E site-directed mutagenesis Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.5 1-Benzylimidazole weak inhibition; weak inhibition Homo sapiens
2.3.2.5 1-vinylimidazole weak inhibition; weak inhibition Homo sapiens
2.3.2.5 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
2.3.2.5 N-omega-acetylhistamine weak inhibition; weak inhibition Homo sapiens
2.3.2.5 PBD150
-
 Homo sapiens
2.3.2.5 PQ912
-
 Homo sapiens
2.3.2.5 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.2.5 additional information
-
 additional information Michaelis-Menten kinetics Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.2.5 extracellular secretory isozyme Homo sapiens
-
-
2.3.2.5 Golgi apparatus
-
 Homo sapiens 5794
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.3.2.5 Zn2+ required for catalysis Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.2.5 L-glutaminyl-peptide Homo sapiens
-
 5-oxoprolyl-peptide + NH3
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.5 Homo sapiens Q16769
-
-
2.3.2.5 Homo sapiens Q9NXS2
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.2.5 recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Homo sapiens
2.3.2.5 recombinant His-tagged wild-type enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.5 L-glutaminyl-peptide
-
 Homo sapiens 5-oxoprolyl-peptide + NH3
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.2.5 glutaminyl cyclase
-
 Homo sapiens
2.3.2.5 Golgi resident glutaminyl cyclase
-
 Homo sapiens
2.3.2.5 gQC
-
 Homo sapiens
2.3.2.5 hQC
-
 Homo sapiens
2.3.2.5 secretory glutaminyl cyclase
-
 Homo sapiens
2.3.2.5 sQC
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.2.5 25
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.2.5 8
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.2.5 additional information
-
 additional information inhibition kinetics Homo sapiens
2.3.2.5 0.00002
-
 SEN177 pH 8.0, 25°C, with enzyme mutant Y115E/Y117E Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.2.5 0.0000247
-
 pH 8.0, 25°C Homo sapiens PQ912
2.3.2.5 0.00005
-
 pH 8.0, 25°C, with enzyme mutant Y115E/Y117E Homo sapiens SEN177