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Literature summary for 2.4.1.17 extracted from
- UDP-glycosyltransferase 3A metabolism of polycyclic aromatic hydrocarbons potential importance in aerodigestive tract tissues (2020), Drug Metab. Dispos., 48, 160-168 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| gene UGT3A1, functional recombinant overexpression of His-tagged isozyme in HEK-293 cells, subcloning in Escherichia coli TOP10 cells | Homo sapiens |
| gene UGT3A2, recombinant overexpression in HEK-293 cells | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
| additional information | - |
additional information | Michaelis-Menten kinetics, kinetic parameters are determined for UGT3A2 using UDP-Glc or UDP-Xyl as cosubstrates | Homo sapiens | |
| 0.0012 | - |
1-hydroxy-pyrene | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens |  |
| 0.0033 | - |
1-hydroxy-pyrene | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0061 | - |
1-hydroxy-benzo[a]pyrene | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0072 | - |
3-hydroxy-benzo[a]pyrene | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0075 | - |
3-hydroxy-benzo[a]pyrene | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0078 | - |
7-hydroxy-benzo[a]pyrene | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0085 | - |
7-hydroxy-benzo[a]pyrene | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.0096 | - |
9-hydroxy-benzo[a]pyrene | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.011 | - |
1-hydroxy-benzo[a]pyrene | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.012 | - |
9-hydroxy-benzo[a]pyrene | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.096 | - |
dibenzo[a,1]pyrene-11,12-diol | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.12 | - |
benzo[a]pyrene-9,10-diol | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.124 | - |
5-methylchrysene-1,2-diol | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.129 | - |
1-naphthol | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.143 | - |
dibenzo[a,1]pyrene-11,12-diol | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.168 | - |
Benzo[a]pyrene-7,8-diol | with UDP-D-xylose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.19 | - |
benzo[a]pyrene-9,10-diol | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.225 | - |
1-naphthol | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 0.397 | - |
Benzo[a]pyrene-7,8-diol | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
| 1.25 | - |
5-methylchrysene-1,2-diol | with UDP-D-glucose, recombinant enzyme in microsomes, pH 7.4, 37°C | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| membrane | - |
Homo sapiens | 16020 | - |
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDP-glucuronate + acceptor | Homo sapiens | - |
UDP + acceptor beta-D-glucuronoside | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q3SY77 | - |
- |
| Homo sapiens | Q6NUS8 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| microsome preparation from wild-type and UGT3A1-overexpressing HEK-293 cells | Homo sapiens |
| microsome preparation from wild-type and UGT3A2-overexpressing HEK-293 cells | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| aerodigestive tract | - |
Homo sapiens | - |
| breast | - |
Homo sapiens | - |
| breast | low expression level | Homo sapiens | - |
| colon | - |
Homo sapiens | - |
| colon | low expression level | Homo sapiens | - |
| esophagus | - |
Homo sapiens | - |
| esophagus | very low expression level | Homo sapiens | - |
| HEK-293 cell | - |
Homo sapiens | - |
| jejunum | - |
Homo sapiens | - |
| larynx | - |
Homo sapiens | - |
| liver | high expression level | Homo sapiens | - |
| liver | low expression level | Homo sapiens | - |
| lung | - |
Homo sapiens | - |
| lung | low expression level | Homo sapiens | - |
| additional information | UGT3A1 exhibits the highest expression in liver with lower expression in aerodigestive tract tissues. Tissue expression pattern, overview | Homo sapiens | - |
| additional information | UGT3A2 is well expressed in extrahepatic tissues. Tissue expression pattern, overview | Homo sapiens | - |
| mouth | floor of mouth, high expression level | Homo sapiens | - |
| mouth | floor of mouth, very low expression level | Homo sapiens | - |
| tongue | - |
Homo sapiens | - |
| tonsil | - |
Homo sapiens | - |
| tonsil | very low expression level | Homo sapiens | - |
| trachea | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 1-hydroxy-benzo[a]pyrene + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | benzo[a]pyrenil-1-O-D-glucoside + UDP | - |
? | |
| 1-hydroxy-pyrene + UDP-D-xylose | - |
Homo sapiens | pyrene 1-O-D-xyloside + UDP | - |
? | |
| 1-hydroxypyrene + UDP-D-glucose | - |
Homo sapiens | pyrene 1-O-D-glucoside + UDP | - |
? | |
| 1-hydroxypyrene + UDP-glucuronate | - |
Homo sapiens | pyrene 1-O-glucuronide + UDP | - |
? | |
| 1-hydroxypyrene + UDP-N-acetylglucosamine | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | pyrenil-1-O-(N-acetylglucosaminide) + UDP | - |
? | |
| 1-naphthol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | naphthyl-1-O-D-glucoside + UDP | - |
? | |
| 3-hydroxy-benzo[a]pyrene + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | benzo[a]pyrenil-3-O-D-glucoside + UDP | - |
? | |
| 5-methylchrysene-1,2-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 1-hydroxy-5-methylchrysene-2-O-D-glucoside + UDP | - |
? | |
| 5-methylchrysene-1,2-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 2-hydroxy-5-methylchrysene-1-O-D-glucoside + UDP | - |
? | |
| 5-methylchrysene-1,2-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 1-hydroxy-5-methylchrysene-2-O-D-xyloside + UDP | - |
? | |
| 5-methylchrysene-1,2-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 2-hydroxy-5-methylchrysene-1-O-D-xyloside + UDP | - |
? | |
| 7-hydroxy-benzo[a]pyrene + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | benzo[a]pyrenil-7-O-D-glucoside + UDP | - |
? | |
| 8-hydroxy-benzo[a]pyrene + UDP-glucuronate | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | benzo[a]pyrenil-8-O-glucuronide + UDP | - |
? | |
| 9-hydroxy-benzo[a]pyrene + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | benzo[a]pyrenil-9-O-D-glucoside + UDP | - |
? | |
| benzo[a]pyrene-7,8-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 7-hydroxy-benzo[a]pyrene-8-O-D-glucoside + UDP | - |
? | |
| benzo[a]pyrene-7,8-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 8-hydroxy-benzo[a]pyrene-7-O-D-glucoside + UDP | - |
? | |
| benzo[a]pyrene-7,8-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 7-hydroxy-benzo[a]pyrene-8-O-D-xyloside + UDP | - |
? | |
| benzo[a]pyrene-7,8-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 8-hydroxy-benzo[a]pyrene-7-O-D-xyloside + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 10-hydroxy-benzo[a]pyrene-9-O-D-glucoside + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 9-hydroxy-benzo[a]pyrene-10-O-D-glucoside + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 10-hydroxy-benzo[a]pyrene-9-O-D-xyloside + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 9-hydroxy-benzo[a]pyrene-10-O-D-xyloside + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-glucuronate | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | 10-hydroxy-benzo[a]pyrene-9-O-glucuronide + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-glucuronate | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | 9-hydroxy-benzo[a]pyrene-10-O-glucuronide + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-N-acetylglucosamine | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | 10-hydroxybenzo[a]pyrene 9-O-(N-acetylglucosaminide) + UDP | - |
? | |
| benzo[a]pyrene-9,10-diol + UDP-N-acetylglucosamine | activity of only UGT3A1-overexpressing microsomes, not wild-type cell microsomes | Homo sapiens | 9-hydroxybenzo[a]pyrene 10-O-(N-acetylglucosaminide) + UDP | - |
? | |
| dibenzo[a,1]pyrene-11,12-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 11-hydroxy-benzo[a]pyrene-12-O-D-glucoside + UDP | - |
? | |
| dibenzo[a,1]pyrene-11,12-diol + UDP-D-glucose | UGT3A2-overexpressing microsomes | Homo sapiens | 12-hydroxy-benzo[a]pyrene-11-O-D-glucoside + UDP | - |
? | |
| dibenzo[a,1]pyrene-11,12-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 11-hydroxy-benzo[a]pyrene-12-O-D-xyloside + UDP | - |
? | |
| dibenzo[a,1]pyrene-11,12-diol + UDP-D-xylose | UGT3A2-overexpressing microsomes | Homo sapiens | 12-hydroxy-benzo[a]pyrene-11-O-D-glucoside + UDP | - |
? | |
| additional information | isozyme UGT3A1 can also use UDP-N-acetylglucosamine as cosubstrate. UGT3A1-overexpressing microsomes also demonstrates activity against 8-hydroxy-benzo[a]pyrene (8-OH-BaP) and BaP-9,10-diol. Two GlcNAc conjugates are observed for BaP-9,10-diol, likely representing N-acetylglucosaminides at the 9- and 10-diol positions. No detectable glycosylation activity for any other PAH tested is seen with UGT3A1-overexpressing microsomes. No glycosylation is observed for microsomes from the parent HEK293 cell line for 1-OH-pyrene, 8-OH-BaP, or BaP-9,10-diol using UDP-GlcNAc as cosubstrate or when using either UDP-Glc, UDP-Xyl, or UDP-GlcUA as cosubstrate | Homo sapiens | ? | - |
- |
|
| additional information | UGT3A2 exhibits glycosylation activity against all of the simple and complex polycyclic aromatic hydrocarbons (PAHs)tested. Isozyme UGT3A2 can also use UDP-D-glucose and UDP-D-xylose as cosubstrates. After screening for activity against the PAH substrates, kinetic parameters are determined for UGT3A2 using UDP-Glc or UDPXyl as cosubstrates | Homo sapiens | ? | - |
- |
|
| UDP-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| UGT3A1 | - |
Homo sapiens |
| UGT3A2 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
General Information
| General Information | Comment | Organism |
|---|---|---|
| evolution | UGT3A enzymes are functionally distinct from other UGT subfamilies (which use UDP-glucuronic acid as a cosubstrate) due to their utilization of alternative cosubstrates (UDP-N-acetylglucosamine for UGT3A1, and UDP-glucose and UDP-xylose for UGT3A2). The overall expression level in tissue is higher for isozyme UGT3A2 compared to isozyme UGT3A1 | Homo sapiens |
| malfunction | UGT3A1-overexpressing microsomes also demonstrates activity against 8-hydroxy-benzo[a]pyrene (8-OH-BaP) and BaP-9,10-diol. Two GlcNAc conjugates are observed for BaP-9,10-diol, likely representing N-acetylglucosaminides at the 9- and 10-diol positions. No detectable glycosylation activity for any other PAH tested is seen with UGT3A1-overexpressing microsomes | Homo sapiens |
| malfunction | UGT3A2-overexpressing microsomes show UGT3A2 activity against all of the PAHs tested using UDP-Glc as cosubstrate. In addition to 1-OH-pyrene, UGT3A2-overexpressing microsomes exhibit high activity against the simple PAHs (1-OH-BaP, 3-OH-BaP, 7-OH-BaP, and 9-OH-BaP) to form glucoside metabolites | Homo sapiens |
| physiological function | polycyclic aromatic hydrocarbons (PAHs) are potent carcinogens and are a primary risk factor for the development of lung and other aerodigestive tract cancers in smokers. The detoxification of PAHs by glucuronidation is well-characterized for the UDP-glycosyltransferase (UGT) 1A, 2A, and 2B subfamilies | Homo sapiens |
| physiological function | polycyclic aromatic hydrocarbons (PAHs) are potent carcinogens and are a primary risk factor for the development of lung and other aerodigestive tract cancers in smokers. The detoxification of PAHs by glucuronidation is well-characterized for the UDP-glycosyltransferase (UGT) 1A, 2A, and 2B subfamilies. UGT3A2 is highly active against PAHs with either UDP-glucose or UDP-xylose as a cosubstrate: UGT3A2 plays an important role in the detoxification of PAHs in aerodigestive tract tissues, and that there may be cosubstrate-dependent differences in the detoxification of PAHs by UGT3A2 | Homo sapiens |
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