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Literature summary for 2.3.2.5 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
Search for more literature for 2.3.2.5

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16769
-
-
Mus musculus Q9CYK2
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
glutaminyl cyclase
-
 Homo sapiens
glutaminyl cyclase
-
 Mus musculus

Ki Value [mM]

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