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Literature summary extracted from

  • Tachibana, M.; Tanaka, M.; Masubuchi, Y.; Horie, T.
    Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes (2005), Drug Metab. Dispos., 33, 803-811.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 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
2.4.1.17 Mefenamic acid specific for isozyme UGT1A9, strong inhibition of grepafloxacin glucuronidation, weak inhibition of levofloxacin, sitafloxacin and moxifloxacin glucuronidation Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 1.9
-
 Sitafloxacin isozyme UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 1.9
-
 moxifloxacin liver microsomes, pH 7.4, 37°C Homo sapiens
2.4.1.17 2.1
-
 grepafloxacin isozyme UGT1A9, pH 7.4, 37°C Homo sapiens
2.4.1.17 2.1
-
 moxifloxacin isozyme UGT1A9, pH 7.4, 37°C Homo sapiens
2.4.1.17 2.6
-
 levofloxacin isozyme UGT1A9, pH 7.4, 37°C Homo sapiens
2.4.1.17 2.7
-
 grepafloxacin isozyme UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 3.4
-
 moxifloxacin isozyme UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 3.7
-
 Sitafloxacin liver microsomes, pH 7.4, 37°C Homo sapiens
2.4.1.17 5.2
-
 grepafloxacin liver microsomes, pH 7.4, 37°C Homo sapiens
2.4.1.17 6
-
 levofloxacin isozyme UGT1A1, pH 7.4, 37°C Homo sapiens
2.4.1.17 6.3
-
 Sitafloxacin isozyme UGT1A9, pH 7.4, 37°C Homo sapiens
2.4.1.17 10
-
 levofloxacin liver microsomes, pH 7.4, 37°C Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.4.1.17 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.1.17 additional information Homo sapiens the enzyme is involved acyl glucuronidation, an important metabolic pathway for fluoroquinolone antobiotics ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens O60656 isozyme UGT1A9; isozyme UGT1A9
-
2.4.1.17 Homo sapiens P22309 isozyme UGT1A1; isozyme UGT1A1
-
2.4.1.17 Homo sapiens P35503 isozyme UGT1A3; isozyme UGT1A3
-
2.4.1.17 Homo sapiens Q9HAW7 isozyme UGT1A7; isozyme UGT1A7
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.17 liver
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.4.1.17 additional information
-
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 additional information the enzyme is involved acyl glucuronidation, an important metabolic pathway for fluoroquinolone antobiotics Homo sapiens ?
-
 ?
2.4.1.17 additional information substrate specificty of isozymes of the 1A subfamily Homo sapiens ?
-
 ?
2.4.1.17 UDP-glucuronate + beta-estradiol
-
 Homo sapiens UDP + estradiol 3-beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + grepafloxacin
-
 Homo sapiens UDP + grepafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + grepafloxacin high activity with isozyme UGT1A9 Homo sapiens UDP + grepafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + grepafloxacin low activity with isozyme UGT1A1 Homo sapiens UDP + grepafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + grepafloxacin low activity with isozyme UGT1A3 Homo sapiens UDP + grepafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + levofloxacin high activity with isozyme UGT1A1 Homo sapiens UDP + levofloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + levofloxacin high activity with isozyme UGT1A3 Homo sapiens UDP + levofloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + levofloxacin high activity with isozyme UGT1A7 Homo sapiens UDP + levofloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + levofloxacin high activity with isozyme UGT1A9 Homo sapiens UDP + levofloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + moxifloxacin high activity with isozyme UGT1A1 Homo sapiens UDP + moxifloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + moxifloxacin low activity with isozyme UGT1A7 Homo sapiens UDP + moxifloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + moxifloxacin low activity with isozyme UGT1A9 Homo sapiens UDP + moxifloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + moxifloxacin very low activity with isozyme UGT1A3 Homo sapiens UDP + moxifloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + propofol
-
 Homo sapiens UDP + propofol beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + sitafloxacin high activity with isozyme UGT1A1 Homo sapiens UDP + sitafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + sitafloxacin high activity with isozyme UGT1A9 Homo sapiens UDP + sitafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + sitafloxacin low activity with isozyme UGT1A3 Homo sapiens UDP + sitafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + sitafloxacin low activity with isozyme UGT1A7 Homo sapiens UDP + sitafloxacin beta-D-glucuronide
-
 ?
2.4.1.17 UDP-glucuronate + trifluoroperazine
-
 Homo sapiens UDP + trifluoroperazine beta-D-glucuronide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 More isozyme of the 1A subfamily Homo sapiens
2.4.1.17 More isozymes of the 1A subfamily Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase
-
 Homo sapiens
2.4.1.17 UGT
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.17 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.17 7.4
-
 assay at Homo sapiens