Application | Comment | Organism |
---|---|---|
medicine | the UGT1A6 splice variant isoform 2, detected in the liver and kidney, has no transferase activity for deferiprone. When UGT1A6_i2 is coexpressed with the classic UGT1A6_i1 isoform, velocity is reduced for deferiprone but remains similar for 4-nitrophenol or serotonin glucuronidation | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | genetic variants UGT1A6*2 with residues A7A181S184, UGT1A6*3 with residue A7, UGT1A6*4 with residues A7S184, and UGT1A6*5 with resiude A181 show Km values similar to reference variant UGT1A6*1, but their Vmax values are reduced by 25% to 70% | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-nitrophenol | competitive | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.73 | - |
4-nitrophenol | pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 | Homo sapiens | |
0.77 | - |
4-nitrophenol | pH 7.5, 37°C, genetic variant UGT1A6*1 | Homo sapiens | |
7.4 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*3 | Homo sapiens | |
8.2 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*2 | Homo sapiens | |
8.2 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*4 | Homo sapiens | |
8.2 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*5 | Homo sapiens | |
9.8 | - |
serotonin | pH 7.5, 37°C, genetic variant UGT1A6*1 | Homo sapiens | |
9.9 | - |
serotonin | pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 | Homo sapiens | |
10 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*1 | Homo sapiens | |
19.3 | - |
deferiprone | pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoform UGT1A6 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
ileum | - |
Homo sapiens | - |
jejunum | - |
Homo sapiens | - |
kidney | - |
Homo sapiens | - |
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-nitrophenol + UDP-glucuronate | - |
Homo sapiens | 4-nitrophenyl beta-D-glucuronide + UDP | - |
? | |
deferiprone + UDP-glucuronate | - |
Homo sapiens | deferiprone 3-O-glucuronide + UDP | - |
? | |
serotonin + UDP-glucuronate | - |
Homo sapiens | UDP + 3-(2-aminoethyl)-1H-indol-5-yl beta-D-glucuronide | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
23.4 | - |
4-nitrophenol | pH 7.5, 37°C, genetic variant UGT1A6*1 | Homo sapiens | |
51.2 | - |
4-nitrophenol | pH 7.5, 37°C, genetic variant UGT1A6*1, co-expression of splice variants i1 and i2 | Homo sapiens |