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Literature summary for 1.14.11.16 extracted from
- Synthesis of novel pyridine-carboxylates as small-molecule inhibitors of human aspartate/asparagine-beta-hydroxylase (2020), ChemMedChem, 15, 1139-1149 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| N-terminally His6-tagged human AspH315-758 (His6-AspH315-758) was produced in Escherichia coli BL21 (DE3) cells using a pET-28a(+) vector | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-((3-phenylpropyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-((4-(trifluoromethyl)benzyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-((4-chlorophenethyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-((4-methoxybenzyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-((4-phenylbutyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-((cyclohexylmethyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-aminoanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-carboxyanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-fluoroanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-methoxyanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-methylanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(2-nitroanilino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(benzylamino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-(phenethylamino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-anilinopyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| 3-[2-(methylsulfanyl)anilino]pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| pyridine-2,3-dicarboxylic acid | - |
Homo sapiens |  |
| pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| pyridine-2,6-dicarboxylic acid | - |
Homo sapiens | |
| rac-3-((1-phenylethyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens | |
| rac-3-((1-phenylpropyl)amino)pyridine-2,4-dicarboxylic acid | - |
Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q12797 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
- |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| additional information | the enzyme is present on the cell surface of invasive cancer cells | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| peptide-L-aspartate + 2-oxoglutarate + O2 | the enzyme accepts epidermal growth factor-like domain (EGFD) substrates with a noncanonical (i. e., Cys 1-2, 3-4, 5-6) disulfide pattern. Synthetic thioether linked cyclic peptide, hFX-CP101-119 is used as substrate. hFX-CP101-119 is designed based on 19 EGFD1 amino acid residues of the sequence of human coagulation factor X (hFX amino acids 101-119) | Homo sapiens | peptide-3-hydroxy-L-aspartate + succinate + CO2 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| aspartate/asparagine-beta-hydroxylase | - |
Homo sapiens |
| ASPH | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00003 | - |
pH 7.5, 20°C | Homo sapiens | pyridine-2,4-dicarboxylic acid | |
| 0.00028 | - |
pH 7.5, 20°C | Homo sapiens | rac-3-((1-phenylethyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.00051 | - |
pH 7.5, 20°C | Homo sapiens | pyridine-2,3-dicarboxylic acid | |
| 0.00058 | - |
pH 7.5, 20°C | Homo sapiens | 3-((4-methoxybenzyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.00122 | - |
pH 7.5, 20°C | Homo sapiens | rac-3-((1-phenylpropyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.00186 | - |
pH 7.5, 20°C | Homo sapiens | 3-((4-(trifluoromethyl)benzyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.00367 | - |
pH 7.5, 20°C | Homo sapiens | 3-((4-chlorophenethyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.00395 | - |
pH 7.5, 20°C | Homo sapiens | 3-(benzylamino)pyridine-2,4-dicarboxylic acid | |
| 0.00467 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-aminoanilino)pyridine-2,4-dicarboxylic acid | |
| 0.00548 | - |
pH 7.5, 20°C | Homo sapiens | pyridine-2,6-dicarboxylic acid | |
| 0.00766 | - |
pH 7.5, 20°C | Homo sapiens | 3-(phenethylamino)pyridine-2,4-dicarboxylic acid | |
| 0.0104 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-carboxyanilino)pyridine-2,4-dicarboxylic acid | |
| 0.0108 | - |
pH 7.5, 20°C | Homo sapiens | 3-((4-phenylbutyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.0109 | - |
pH 7.5, 20°C | Homo sapiens | 3-((3-phenylpropyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.0129 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-methylanilino)pyridine-2,4-dicarboxylic acid | |
| 0.0131 | - |
pH 7.5, 20°C | Homo sapiens | 3-((cyclohexylmethyl)amino)pyridine-2,4-dicarboxylic acid | |
| 0.0138 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-methoxyanilino)pyridine-2,4-dicarboxylic acid | |
| 0.0161 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-nitroanilino)pyridine-2,4-dicarboxylic acid | |
| 0.0161 | - |
pH 7.5, 20°C | Homo sapiens | 3-[2-(methylsulfanyl)anilino]pyridine-2,4-dicarboxylic acid | |
| 0.0221 | - |
pH 7.5, 20°C | Homo sapiens | 3-(2-fluoroanilino)pyridine-2,4-dicarboxylic acid | |
| 0.0388 | - |
pH 7.5, 20°C | Homo sapiens | 3-anilinopyridine-2,4-dicarboxylic acid |
General Information
| General Information | Comment | Organism |
|---|---|---|
| drug target | the enzyme is a potential medicinal chemistry target for anticancer therapy | Homo sapiens |
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