Cloned (Comment) | Organism |
---|---|
expressed in Pichia pastoris strain X33 | Homo sapiens |
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 | 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16769 | - |
- |
Mus musculus | Q9CYK2 | - |
- |
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 | Comment | Organism |
---|---|---|
glutaminyl cyclase | - |
Homo sapiens |
glutaminyl cyclase | - |
Mus musculus |
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 |