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Literature summary extracted from

  • Koch, B.; Buchholz, M.; Wermann, M.; Heiser, U.; Schilling, S.; Demuth, H.U.
    Probing secondary glutaminyl cyclase (QC) inhibitor interactions applying an in silico-modeling/site-directed mutagenesis approach: implications for drug development (2012), Chem. Biol. Drug Des., 80, 937-946.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.2.5 expressed in Pichia pastoris strain X33 Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.3.2.5 F325A the mutant shows a 190fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 F325N the mutant shows a 815fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 F325Y the mutant shows a 381fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 I303A the mutation results in a 66.3fold increase in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 I303F the mutation results in a 6.2fold increase in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 I303N the mutation results in a 112fold increase in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 I303V the mutation results in a 1.9fold increase in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 K144A the mutant shows a 1.21fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 K144M the mutant shows a 335fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 K144R the mutant shows a 237fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 S323A the mutation leads to a significant decrease (0.2fold) in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 S323T the mutation leads to a significant decrease (0.21fold) in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 S323V the mutation leads to a strong decrease (0.074fold) in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 W329F the mutation leads to a significant decrease (0.56fold) in the Ki value of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 W329Y the mutation does not affect the Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 Y299A the mutant shows a 122fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens
2.3.2.5 Y299F the mutant shows a 220fold increase in Ki of PBD150 compared to the wild type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.5 benzimidazole
-
 Homo sapiens
2.3.2.5 benzimidazole
-
 Mus musculus
2.3.2.5 cysteamine
-
 Homo sapiens
2.3.2.5 cysteamine
-
 Mus musculus
2.3.2.5 imidazole
-
 Homo sapiens
2.3.2.5 imidazole
-
 Mus musculus
2.3.2.5 PBD150 potent inhibitor Homo sapiens
2.3.2.5 PBD150 potent inhibitor Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.5 Homo sapiens Q16769
-
-
2.3.2.5 Mus musculus Q9CYK2
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.5 L-Gln-2-naphthylamide
-
 Homo sapiens 5-oxoprolyl-2-naphthylamide + NH3
-
 ?
2.3.2.5 L-Gln-2-naphthylamide
-
 Mus musculus 5-oxoprolyl-2-naphthylamide + NH3
-
 ?
2.3.2.5 L-Gln-7-amido-4-methylcoumarin
-
 Homo sapiens 5-oxoprolyl-7-amido-4-methylcoumarin + NH3
-
 ?
2.3.2.5 L-Gln-7-amido-4-methylcoumarin
-
 Mus musculus 5-oxoprolyl-7-amido-4-methylcoumarin + NH3
-
 ?
2.3.2.5 L-Gln-Gly
-
 Homo sapiens 5-oxoprolyl-Gly + NH3
-
 ?
2.3.2.5 L-Gln-Gly
-
 Mus musculus 5-oxoprolyl-Gly + NH3
-
 ?
2.3.2.5 L-Gln-L-Lys-L-Arg-L-Leu-NH2
-
 Homo sapiens 5-oxoprolyl-L-Lys-L-Arg-L-Leu-NH2 + NH3
-
 ?
2.3.2.5 L-Gln-L-Lys-L-Arg-L-Leu-NH2
-
 Mus musculus 5-oxoprolyl-L-Lys-L-Arg-L-Leu-NH2 + NH3
-
 ?
2.3.2.5 L-Gln-L-Phe-L-Ala-NH2
-
 Homo sapiens 5-oxoprolyl-L-Phe-L-Ala-NH2 + NH3
-
 ?
2.3.2.5 L-Gln-L-Phe-L-Ala-NH2
-
 Mus musculus 5-oxoprolyl-L-Phe-L-Ala-NH2 + NH3
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.2.5 glutaminyl cyclase
-
 Homo sapiens
2.3.2.5 glutaminyl cyclase
-
 Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.2.5 0.0001
-
 PBD150 wild type enzyme, in 50 mM Tris, pH 8.0, at 30°C Homo sapiens
2.3.2.5 0.000114
-
 PBD150 wild type enzyme, in 50 mM Tris, pH 8.0, at 30°C Mus musculus