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Literature summary extracted from

  • Wen, Z.; Tallman, M.N.; Ali, S.Y.; Smith, P.C.
    UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics (2007), Drug Metab. Dispos., 35, 371-380.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 17alpha-ethinylestradiol strongly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.0 42 mM) but shows very similar and moderate inhibition on etoposide phenolic glucuronide (IC50: 0.2 mM) and etoposide alcoholic glucuronide EAG1 (IC50: 0.21 mM) Homo sapiens
2.4.1.17 beta-estradiol exhibits strong inhibition on etoposide phenolic glucuronide (IC50: 0.068 mM) and etoposide alcoholic glucuronide EAG2 (IC50: 0.086 mM). The inhibitory effect of beta-estradiol on the formation of etoposide alcoholic glucuronide EAG1 is not so significant in comparison with the other two etoposide glucuronide isomers, even at very high concentration of beta-estradiol (about 80% at 2 mM) Homo sapiens
2.4.1.17 bilirubin strongly inhibits the formation of etoposide phenolic glucuronide (IC50: 0.075 mM) and EAG1 (I50: 0.054 mM), and significantly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.140 mM) Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 microsome
-
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 etoposide + UDP-glucuronate Homo sapiens UGT1A1 is principally responsible for the formation of etoposide glucuronides, mainly in the form of phenolic glucuronide UDP + etoposide glucuronide
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens P22309
-
-
2.4.1.17 Homo sapiens P35503
-
-
2.4.1.17 Homo sapiens Q9HAW9
-
-

Source Tissue

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.17 etoposide + UDP-glucuronate
-
Homo sapiens UDP + etoposide glucuronide
-
?
2.4.1.17 etoposide + UDP-glucuronate UGT1A1 is principally responsible for the formation of etoposide glucuronides, mainly in the form of phenolic glucuronide Homo sapiens UDP + etoposide glucuronide
-
?
2.4.1.17 etoposide + UDP-glucuronate activity with UGT1A3 is much lower than activity with UGT1A1 Homo sapiens UDP + etoposide glucuronide
-
?
2.4.1.17 etoposide + UDP-glucuronate activity with UGT1A8 is much lower than activity with UGT1A1 Homo sapiens UDP + etoposide glucuronide
-
?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP-glucuronosyltransferase 1A1
-
Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase 1A3
-
Homo sapiens
2.4.1.17 UDP-glucuronosyltransferase 1A8
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.1.17 0.042
-
strongly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.042 mM) Homo sapiens 17alpha-ethinylestradiol
2.4.1.17 0.054
-
strongly inhibits EAG1 (I50: 0.054 mM) Homo sapiens bilirubin
2.4.1.17 0.068 0.086 exhibits strong inhibition on etoposide phenolic glucuronide (IC50: 0.068 mM) and etoposide alcoholic glucuronide EAG2 (IC50: 0.086 mM). The inhibitory effect of beta-estradiol on the formation of etoposide alcoholic glucuronide EAG1 is not so significant Homo sapiens beta-estradiol
2.4.1.17 0.075
-
strongly inhibits the formation of etoposide phenolic glucuronide (IC50: 0.075 mM) Homo sapiens bilirubin
2.4.1.17 0.14
-
significantly inhibits the formation of etoposide alcoholic glucuronide EAG2 (IC50: 0.140 mM) Homo sapiens bilirubin
2.4.1.17 0.2
-
shows very similar and moderate inhibition on etoposide phenolic glucuronide (IC50: 0.2 mM) Homo sapiens 17alpha-ethinylestradiol
2.4.1.17 0.21
-
shows very similar and moderate inhibition on etoposide alcoholic glucuronide EAG1 (IC50: 0.21 mM) Homo sapiens 17alpha-ethinylestradiol