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Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Inhibitors

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 [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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

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

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

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 [°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