Inhibitors | Comment | Organism | Structure |
---|---|---|---|
bilirubin | specific for isozyme UGT1A1, strong inhibition of sitafloxacin and moxifloxacin glucuronidation, moderate inhibition of levofloxacin glucuronidation, and weak inhibition of grepafloxacin glucuronidation | Homo sapiens | |
Mefenamic acid | specific for isozyme UGT1A9, strong inhibition of grepafloxacin glucuronidation, weak inhibition of levofloxacin, sitafloxacin and moxifloxacin glucuronidation | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.9 | - |
Sitafloxacin | isozyme UGT1A1, pH 7.4, 37°C | Homo sapiens | |
1.9 | - |
moxifloxacin | liver microsomes, pH 7.4, 37°C | Homo sapiens | |
2.1 | - |
grepafloxacin | isozyme UGT1A9, pH 7.4, 37°C | Homo sapiens | |
2.1 | - |
moxifloxacin | isozyme UGT1A9, pH 7.4, 37°C | Homo sapiens | |
2.6 | - |
levofloxacin | isozyme UGT1A9, pH 7.4, 37°C | Homo sapiens | |
2.7 | - |
grepafloxacin | isozyme UGT1A1, pH 7.4, 37°C | Homo sapiens | |
3.4 | - |
moxifloxacin | isozyme UGT1A1, pH 7.4, 37°C | Homo sapiens | |
3.7 | - |
Sitafloxacin | liver microsomes, pH 7.4, 37°C | Homo sapiens | |
5.2 | - |
grepafloxacin | liver microsomes, pH 7.4, 37°C | Homo sapiens | |
6 | - |
levofloxacin | isozyme UGT1A1, pH 7.4, 37°C | Homo sapiens | |
6.3 | - |
Sitafloxacin | isozyme UGT1A9, pH 7.4, 37°C | Homo sapiens | |
10 | - |
levofloxacin | liver microsomes, pH 7.4, 37°C | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | the enzyme is involved acyl glucuronidation, an important metabolic pathway for fluoroquinolone antobiotics | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60656 | isozyme UGT1A9; isozyme UGT1A9 | - |
Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
Homo sapiens | P35503 | isozyme UGT1A3; isozyme UGT1A3 | - |
Homo sapiens | Q9HAW7 | isozyme UGT1A7; isozyme UGT1A7 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
additional information | - |
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | the enzyme is involved acyl glucuronidation, an important metabolic pathway for fluoroquinolone antobiotics | Homo sapiens | ? | - |
? | |
additional information | substrate specificty of isozymes of the 1A subfamily | Homo sapiens | ? | - |
? | |
UDP-glucuronate + beta-estradiol | - |
Homo sapiens | UDP + estradiol 3-beta-D-glucuronide | - |
? | |
UDP-glucuronate + grepafloxacin | - |
Homo sapiens | UDP + grepafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + grepafloxacin | high activity with isozyme UGT1A9 | Homo sapiens | UDP + grepafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + grepafloxacin | low activity with isozyme UGT1A1 | Homo sapiens | UDP + grepafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + grepafloxacin | low activity with isozyme UGT1A3 | Homo sapiens | UDP + grepafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + levofloxacin | high activity with isozyme UGT1A1 | Homo sapiens | UDP + levofloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + levofloxacin | high activity with isozyme UGT1A3 | Homo sapiens | UDP + levofloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + levofloxacin | high activity with isozyme UGT1A7 | Homo sapiens | UDP + levofloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + levofloxacin | high activity with isozyme UGT1A9 | Homo sapiens | UDP + levofloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + moxifloxacin | high activity with isozyme UGT1A1 | Homo sapiens | UDP + moxifloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + moxifloxacin | low activity with isozyme UGT1A7 | Homo sapiens | UDP + moxifloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + moxifloxacin | low activity with isozyme UGT1A9 | Homo sapiens | UDP + moxifloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + moxifloxacin | very low activity with isozyme UGT1A3 | Homo sapiens | UDP + moxifloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + propofol | - |
Homo sapiens | UDP + propofol beta-D-glucuronide | - |
? | |
UDP-glucuronate + sitafloxacin | high activity with isozyme UGT1A1 | Homo sapiens | UDP + sitafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + sitafloxacin | high activity with isozyme UGT1A9 | Homo sapiens | UDP + sitafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + sitafloxacin | low activity with isozyme UGT1A3 | Homo sapiens | UDP + sitafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + sitafloxacin | low activity with isozyme UGT1A7 | Homo sapiens | UDP + sitafloxacin beta-D-glucuronide | - |
? | |
UDP-glucuronate + trifluoroperazine | - |
Homo sapiens | UDP + trifluoroperazine beta-D-glucuronide | - |
? |
Synonyms | Comment | Organism |
---|---|---|
More | isozyme of the 1A subfamily | Homo sapiens |
More | isozymes of the 1A subfamily | Homo sapiens |
UDP-glucuronosyltransferase | - |
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 |