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Literature summary for 2.1.3.2 extracted from
- New regulatory mechanism-based inhibitors of aspartate transcarbamoylase for potential anticancer drug development (2020), FEBS J., 287, 3579-3599 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21(DE3) cells | Homo sapiens |
| expressed in Escherichia coli BL21(DE3) cells | Escherichia coli |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| hanging drop vapor diffusion method, using 0.2 m NH4Ac, 0.1 m Tris pH 8.5, 20% (w/v) PEG3350, and 10% glycerol for all enzyme mutants, and 0.1 m HEPES pH 7.0, 30% (w/v) Jeffamine M-600 pH 7.0, and 10% (v/v) glycerol for all enzyme holo mutants | Escherichia coli |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| G128A | the mutation completely abolishes enzyme activity | Escherichia coli |
| G128A/G130A | the mutation completely abolishes enzyme activity | Escherichia coli |
| G128A/G130A | the mutant loses almost all activity | Homo sapiens |
| G130A | the mutant retains some activity | Homo sapiens |
| G132A | the mutation completely abolishes enzyme activity | Homo sapiens |
| G166A | the mutant retains some activity | Homo sapiens |
| G166A | the mutant retains some activity | Escherichia coli |
| G166P | the mutant loses almost all activity | Homo sapiens |
| G166P | the mutant loses almost all activity | Escherichia coli |
| R167A | the mutation completely abolishes enzyme activity | Escherichia coli |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-(3-methyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoate | - |
Escherichia coli |  |
| 4-(3-methyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoate | - |
Homo sapiens | |
| 5-([6-[(2E)-2-([2-[(2,4-dichlorophenyl)methoxy]phenyl]methylidene)hydrazinyl][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]amino)-1,3-dihydro-2H-benzimidazol-2-one | - |
Escherichia coli | |
| 5-([6-[(2E)-2-([2-[(2,4-dichlorophenyl)methoxy]phenyl]methylidene)hydrazinyl][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]amino)-1,3-dihydro-2H-benzimidazol-2-one | - |
Homo sapiens | |
| additional information | not inhibited by fluorouracil | Escherichia coli | |
| additional information | not inhibited by fluorouracil | Homo sapiens | |
| YD19 | - |
Homo sapiens | |
| YD21 | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.7 | - |
Carbamoyl phosphate | pH and temperature not specified in the publication | Homo sapiens | |
| 9.6 | - |
Carbamoyl phosphate | pH and temperature not specified in the publication | Escherichia coli | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| carbamoyl phosphate + L-aspartate | Homo sapiens | - |
phosphate + N-carbamoyl-L-aspartate | - |
? | |
| carbamoyl phosphate + L-aspartate | Escherichia coli | - |
phosphate + N-carbamoyl-L-aspartate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Escherichia coli | P0A786 | - |
- |
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| Ni-NTA column chromatography and Superdex 200 gel filtration | Homo sapiens |
| Ni-NTA column chromatography and Superdex 200 gel filtration | Escherichia coli |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| A-549 cell | - |
Homo sapiens | - |
| HeLa cell | - |
Homo sapiens | - |
| Hep-G2 cell | - |
Homo sapiens | - |
| MCF-7 cell | - |
Homo sapiens | - |
| PC-3 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| carbamoyl phosphate + L-aspartate | - |
Homo sapiens | phosphate + N-carbamoyl-L-aspartate | - |
? | |
| carbamoyl phosphate + L-aspartate | - |
Escherichia coli | phosphate + N-carbamoyl-L-aspartate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aspartate transcarbamoylase | - |
Homo sapiens |
| aspartate transcarbamoylase | - |
Escherichia coli |
| ATCase | - |
Homo sapiens |
| ATCase | - |
Escherichia coli |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0018 | - |
pH and temperature not specified in the publication | Escherichia coli | 5-([6-[(2E)-2-([2-[(2,4-dichlorophenyl)methoxy]phenyl]methylidene)hydrazinyl][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]amino)-1,3-dihydro-2H-benzimidazol-2-one | |
| 0.0041 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-([6-[(2E)-2-([2-[(2,4-dichlorophenyl)methoxy]phenyl]methylidene)hydrazinyl][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]amino)-1,3-dihydro-2H-benzimidazol-2-one | |
| 0.005 | - |
pH and temperature not specified in the publication | Escherichia coli | 4-(3-methyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoate | |
| 0.0154 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(3-methyl-2,4,6-trioxo-2,3,4,5,6,11-hexahydro-1H-indeno[2',1':5,6]pyrido[2,3-d]pyrimidin-5-yl)phenyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoate | |
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