Crystallization (Comment) | Organism |
---|---|
hanging drop vapor-diffusion method. The space group of the crystal is R32, with typical unit cells of a = b = 119 A and c = 333A, in which an asymmetric unit comprises two human glutaminyl cyclase molecules. Crystal structures of the enzyme bound to inhibitors: 1-vinylimidazole, 1-benzylimidazole and N-omega-acetylhistamine | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D248A | no activity | Homo sapiens |
D305L | no activity | Homo sapiens |
E201D | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 200fold lower than wild-type ratio | Homo sapiens |
E201Q | almost no catalytic activity | Homo sapiens |
F146A | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 1.43fold lower than wild-type ratio | Homo sapiens |
F325A | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 4.9fold lower than wild-type ratio | Homo sapiens |
K144A | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 1.7fold lower than wild-type ratio | Homo sapiens |
Q304L | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 1.7fold lower than wild-type ratio | Homo sapiens |
R54W | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 1.4fold lower than wild-type ratio | Homo sapiens |
W207F | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 3.45fold lower than wild-type ratio | Homo sapiens |
W207L | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 56fold lower than wild-type ratio | Homo sapiens |
W329A | the ratio of turnover-number to KM-value for Gln-Gln at pH 8.0 is 297fold lower than wild-type ratio | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-Benzylimidazole | - |
Homo sapiens | |
1-vinylimidazole | - |
Homo sapiens | |
N-omega-acetylhistamine | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.59 | - |
Gln-Gln | pH 8.0, mutant enzyme W207F | Homo sapiens | |
0.63 | - |
Gln-Gln | pH 8.0, wild-type enzyme | Homo sapiens | |
0.76 | - |
Gln-Gln | pH 8.0, mutant enzyme R54W | Homo sapiens | |
0.79 | - |
Gln-Gln | pH 7.0, wild-type enzyme | Homo sapiens | |
0.82 | - |
Gln-Gln | pH 8.0, mutant enzyme F146A | Homo sapiens | |
0.9 | - |
Gln-Gln | pH 7.5, wild-type enzyme | Homo sapiens | |
0.9 | - |
Gln-Gln | pH 8.5, wild-type enzyme | Homo sapiens | |
1.16 | - |
Gln-Gln | pH 8.0, mutant enzyme Q304L | Homo sapiens | |
1.47 | - |
Gln-Gln | pH 8.0, mutant enzyme K144A | Homo sapiens | |
1.77 | - |
Gln-Gln | pH 8.0, mutant enzyme W207L | Homo sapiens | |
2.06 | - |
Gln-Gln | pH 8.8, wild-type enzyme | Homo sapiens | |
4.67 | - |
Gln-Gln | pH 8.0, mutant enzyme F325A | Homo sapiens | |
12.62 | - |
Gln-Gln | pH 8.0, mutant enzyme E201D | Homo sapiens | |
29.53 | - |
Gln-Gln | pH 8.0, mutant enzyme W329A | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Zn2+ | the active site is coordinated to three conserved residues and one water molecule, which is replaced by an imidazole nitrogen upon binding of inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16769 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
bone marrow | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Gln-Gln | - |
Homo sapiens | Glp-Gln + NH3 | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.43 | - |
Gln-Gln | pH 8.0, mutant enzyme W207L | Homo sapiens | |
0.87 | - |
Gln-Gln | pH 8.0, mutant enzyme E201D | Homo sapiens | |
1.35 | - |
Gln-Gln | pH 8.0, mutant enzyme W329A | Homo sapiens | |
2.32 | - |
Gln-Gln | pH 8.0, mutant enzyme W207F | Homo sapiens | |
7.3 | - |
Gln-Gln | pH 7.0, wild-type enzyme | Homo sapiens | |
7.35 | - |
Gln-Gln | pH 8.0, mutant enzyme R54W | Homo sapiens | |
7.91 | - |
Gln-Gln | pH 8.0, mutant enzyme F146A | Homo sapiens | |
8.56 | - |
Gln-Gln | pH 8.8, wild-type enzyme | Homo sapiens | |
8.63 | - |
Gln-Gln | pH 8.0, wild-type enzyme | Homo sapiens | |
9.39 | - |
Gln-Gln | pH 8.0, mutant enzyme Q304L | Homo sapiens | |
9.76 | - |
Gln-Gln | pH 7.5, wild-type enzyme | Homo sapiens | |
9.93 | - |
Gln-Gln | pH 8.5, wild-type enzyme | Homo sapiens | |
11.67 | - |
Gln-Gln | pH 8.0, mutant enzyme K144A | Homo sapiens | |
12.91 | - |
Gln-Gln | pH 8.0, mutant enzyme F325A | Homo sapiens |