Cloned (Comment) | Organism |
---|---|
expression of wild-type and mutant isozymes in Pichia pastoris | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D145A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D150A | site-directed mutagenesis, mutation of isozyme UGT1A6, inactive mutant | Homo sapiens |
D357A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D394A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to slightly reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D397A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D420A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D447A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to highly reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D454A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
D488A | site-directed mutagenesis, mutation of isozyme UGT1A6, inactive mutant | Homo sapiens |
E287A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 1.4fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E289A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 3.2fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E297A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 2.0fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E314A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 7.0fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E378A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 150fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E378D | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
E378S | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
E461A | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to 350fold reduced glucuronidation activity compared to the wild-type enzyme | Homo sapiens |
E461D | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
E461Q | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
E461S | site-directed mutagenesis, mutation of isozyme UGT1A6 leading to reduced glucuronidation activity and altered kinetics compared to the wild-type enzyme | Homo sapiens |
H39P | site-directed mutagenesis, mutation of His39 residue of isozyme UGT1A1 to proline leads to loss of glucuronidation of phenols but not of estrogens | Homo sapiens |
H40P | site-directed mutagenesis, replacing of His40 residue of isozyme UGT1A3 with proline shifts the substrate specificity toward that of isozyme UGT1A4 with loss of glucuronidation of phenolic substrates | Homo sapiens |
P40H | site-directed mutagenesis, replacing Pro-40 of isozyme UGT1A4 by histidine expands the glucuronidation activity of the enzyme to phenolic and carboxylic compounds, therefore, leading to UGT1A3-type isoform in terms of substrate specificity | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | kinetics of wild-type UGT1A6 and mutants, overview | Homo sapiens | |
0.00012 | - |
4-Methylumbelliferone | pH 7.4, 37°C, recombinant wild-type isozyme UGT1A6 | Homo sapiens | |
0.00025 | - |
UDP-D-glucuronate | pH 7.4, 37°C, recombinant wild-type isozyme UGT1A6 | 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 + acceptor | Homo sapiens | - |
UDP + acceptor beta-D-glucuronoside | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P19224 | isozyme UGT1A6; diverse isozymes | - |
Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
Homo sapiens | P22310 | isozyme UGT1A4; diverse isozymes | - |
Homo sapiens | P35503 | isozyme UGT1A3; isozyme UGT1A3 | - |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
UDP-alpha-D-glucuronate + acceptor = UDP + acceptor beta-D-glucuronoside | aspartic acid residues, especially Asp150 and Asp488, and histidine residues mediate the acid-base reaction mechanism and the substrate specificity of the human subfamily of UDP-D-glucuronosyltransferases 1A catalyzing the nucleophilic attack of phenolic xenobiotics on UDP-D-glucuronic acid, leading to the formation of water-soluble glucuronides, overview | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | UGT1A1 substrate specificity, overview | Homo sapiens | ? | - |
? | |
UDP-D-glucuronate + 1-naphthol | isozyme UGT1A1 | Homo sapiens | UDP + 1-naphthyl beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 2-hydroxyestradiol | isozyme UGT1A1 | Homo sapiens | UDP + 2-hydroxyestradiol beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 2-hydroxyestrone | isozyme UGT1A1 | Homo sapiens | UDP + 2-hydroxyestrone beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 4-methylumbelliferone | isozyme UGT1A1 | Homo sapiens | UDP + 4-methylumbelliferone beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 4-methylumbelliferone | isozyme UGT1A6 | Homo sapiens | UDP + 4-methylumbelliferone beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + 4-nitrophenol | isozyme UGT1A1 | Homo sapiens | UDP + 4-nitrophenyl beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + beta-D-estradiol | isozyme UGT1A1 | Homo sapiens | UDP + beta-estradiol 3-O-beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + eugenol | isozyme UGT1A1 | Homo sapiens | UDP + eugenol beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + octylgallate | isozyme UGT1A1 | Homo sapiens | UDP + octylgallate beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + scopoletin | isozyme UGT1A1 | Homo sapiens | UDP + scopoletin beta-D-glucuronoside | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase | - |
Homo sapiens |
UDP-glucuronosyltransferase 1A1 | - |
Homo sapiens |
UGT | - |
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 |