Cloned (Comment) | Organism |
---|---|
expression in HEK-293 cell | Homo sapiens |
expression in insect cell | Homo sapiens |
expression of wild-type isozyme UGT1A10 in insect cells, overview | Homo sapiens |
expression of wild-type isozyme UGT1A7 in insect cells, overview | Homo sapiens |
expression of wild-type isozyme UGT1A8 in insect cells, overview | Homo sapiens |
expression of wild-type isozyme UGT1A9 and mutants in HEK-293 cells, expression of wild-type isozyme UGT1A9 in insect cells, expression levels, overview | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D152A | site-directed mutagenesis, exchange of a conserved residue from isozyme UGT1A9 for the corresponding residue in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9, the mutant is active with the substrate 3-hydroxydesloratadine specific for isozyme UGT1A8 | Homo sapiens |
E241A | site-directed mutagenesis, exchange of a conserved residue from isozyme UGT1A9 for the corresponding residue in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
E241A | replacement of amino acid to corresponding residue of isoform UGT1A8 | Homo sapiens |
K91M/A92D | site-directed mutagenesis, exchange of conserved residues from isozyme UGT1A9 for the corresponding residues in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
K91M/A92D | replacement of amino acid to corresponding residue of isoform UGT1A8 | Homo sapiens |
L173A | site-directed mutagenesis, exchange of a conserved residue from isozyme UGT1A9 for the corresponding residue in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
L173A | replacement of amino acid to corresponding residue of isoform UGT1A8 | Homo sapiens |
L219F/H221Q/R222Y | site-directed mutagenesis, exchange of conserved residues from isozyme UGT1A9 for the corresponding residues in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
L219F/H221Q/R222Y | replacement of amino acid to corresponding residue of isoform UGT1A8 | Homo sapiens |
N152A | replacement of amino acid to corresponding residue of isoform UGT1A8, increase in Km and Vmax values for substrates 4-methylumbelliferone and 4-nitrophenol. Active against substrate 3-hydroxydesloratadine, specifc substrate of isoform UGT1A8 | Homo sapiens |
R42Q | site-directed mutagenesis, exchange of a conserved residue from isozyme UGT1A9 for the corresponding residue in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
R42Q | replacement of amino acid to corresponding residue of isoform UGT1A8, increase in Km value for substrates 4-methylumbelliferone and 4-nitrophenol | Homo sapiens |
Y106F/G111S/D115G | site-directed mutagenesis, exchange of conserved residues from isozyme UGT1A9 for the corresponding residues in isozyme UGT1A8, the mutant shows altered substrate specificity compared to wild-type isozyme UGT1A9 | Homo sapiens |
Y106F/G111S/D115G | replacement of amino acid to corresponding residue of isoform UGT1A8, increase in Vmax value for substrates 4-methylumbelliferone and 4-nitrophenol | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | kinetic analysis of wild-type isozyme UGT1A9 and mutants expressed in HEK293 cells, overview | Homo sapiens | |
0.0021 | - |
4-Methylumbelliferone | mutant L173A, pH 7.4, 37°C | Homo sapiens | |
0.0036 | - |
4-Methylumbelliferone | mutant K91M/A92D, pH 7.4, 37°C | Homo sapiens | |
0.0044 | - |
4-Methylumbelliferone | wild-type, pH 7.4, 37°C | Homo sapiens | |
0.0044 | - |
4-Methylumbelliferone | mutant E241A, pH 7.4, 37°C | Homo sapiens | |
0.0056 | - |
4-Methylumbelliferone | mutant Y106F/G111S/D115G, pH 7.4, 37°C | Homo sapiens | |
0.0059 | - |
4-Methylumbelliferone | mutant L219F/H221Q/R222Y, pH 7.4, 37°C | Homo sapiens | |
0.0091 | - |
4-Methylumbelliferone | mutant N152A, pH 7.4, 37°C | Homo sapiens | |
0.0101 | - |
4-Methylumbelliferone | mutant R42Q, pH 7.4, 37°C | Homo sapiens | |
0.0102 | - |
4-nitrophenol | mutant Y106F/G111S/D115G, pH 7.4, 37°C | Homo sapiens | |
0.0152 | - |
4-nitrophenol | mutant L219F/H221Q/R222Y, pH 7.4, 37°C | Homo sapiens | |
0.0157 | - |
4-nitrophenol | mutant L173A, pH 7.4, 37°C | Homo sapiens | |
0.0169 | - |
4-nitrophenol | wild-type, pH 7.4, 37°C | Homo sapiens | |
0.0178 | - |
4-nitrophenol | mutant K91M/A92D, pH 7.4, 37°C | Homo sapiens | |
0.0188 | - |
4-nitrophenol | mutant E241A, pH 7.4, 37°C | Homo sapiens | |
0.03 | - |
4-nitrophenol | mutant R42Q, pH 7.4, 37°C | Homo sapiens | |
0.0492 | - |
4-nitrophenol | mutant N152A, pH 7.4, 37°C | Homo sapiens | |
0.1917 | - |
4-Methylumbelliferone | isoform UGT1A8, pH 7.4, 37°C | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-D-glucuronate + 3-hydroxydesloratadine | Homo sapiens | specific substrate of isozyme UGT1A8 | UDP + 3-hydroxydesloratadine beta-O-D-glucuronoside | - |
? | |
UDP-D-glucuronate + acceptor | Homo sapiens | the enzyme plays a key role in the metabolism of endogenous and exogenous compounds | UDP + acceptor beta-D-glucuronoside | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoform UGT1A8 | - |
Homo sapiens | - |
isoform UGT1A9 | - |
Homo sapiens | O60656 | isozyme UGT1A9; isozyme UGT1A9 | - |
Homo sapiens | Q9HAW7 | isozyme UGT1A7; isozyme UGT1A7 | - |
Homo sapiens | Q9HAW8 | isozyme UGT1A10; isozyme UGT1A10 | - |
Homo sapiens | Q9HAW9 | isozyme UGT1A8; isozyme UGT1A8 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3-hydroxydesloratadine + UDP-glucuronate | specific substrate of isoform UGT1A8 | Homo sapiens | UDP + 3-hydroxydesloratadinyl-O-glucuronide | - |
? | |
3-hydroxydesloratadine + UDP-glucuronate | specific substrate of isoform UGT1A8, substrate of isoform UGT1A9 mutant N152A | Homo sapiens | UDP + 3-hydroxydesloratadinyl-O-glucuronide | - |
? | |
4-methylumbelliferone + UDP-glucuronate | - |
Homo sapiens | UDP + 4-methylumbelliferyl-7-O-beta-D-glucuronide | - |
? | |
4-nitrophenol + UDP-glucuronate | - |
Homo sapiens | 4-nitrophenyl beta-D-glucuronide + UDP | - |
? | |
additional information | key amino acid residues responsible for the differences in substrate specificity of isozymes UGT1A9 and UGT1A8, overview | Homo sapiens | ? | - |
? | |
additional information | no substrate of isoform UGT1A8: 4-nitrophenol | Homo sapiens | ? | - |
? | |
UDP-D-glucuronate + 3-hydroxydesloratadine | specific substrate of isozyme UGT1A8 | Homo sapiens | UDP + 3-hydroxydesloratadine beta-O-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 4-methylumbelliferone | - |
Homo sapiens | UDP + 4-methylumbelliferyl beta-O-glucuronoside | - |
? | |
UDP-D-glucuronate + 4-nitrophenol | - |
Homo sapiens | UDP + 4-nitrophenyl beta-O-D-glucuronoside | - |
? | |
UDP-D-glucuronate + acceptor | the enzyme plays a key role in the metabolism of endogenous and exogenous compounds | Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? |
Subunits | Comment | Organism |
---|---|---|
dimer | - |
Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase | - |
Homo sapiens |
UGT1A8 | - |
Homo sapiens |
UGT1A9 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |