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Literature summary for 2.3.2.5 extracted from
- Crystal structures of human glutaminyl cyclase, an enzyme responsible for protein N-terminal pyroglutamate formation (2005), Proc. Natl. Acad. Sci. USA, 102, 13117-13122.
Crystallization (Commentary)
| 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
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 1-Benzylimidazole | - |
Homo sapiens |  |
| 1-vinylimidazole | - |
Homo sapiens | |
| N-omega-acetylhistamine | - |
Homo sapiens | |
KM Value [mM]
| 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
| 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
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q16769 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| bone marrow | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Gln-Gln | - |
Homo sapiens | Glp-Gln + NH3 | - |
? | |
Turnover Number [1/s]
| 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 | |
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