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Literature summary extracted from

  • Sun, D.; Sharma, A.K.; Dellinger, R.W.; Blevins-Primeau, A.S.; Balliet, R.M.; Chen, G.; Boyiri, T.; Amin, S.; Lazarus, P.
    Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases (2007), Drug Metab. Dispos., 35, 2006-2014.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 isozyme UGT1A3, DNA and amino acid sequence determination and analysis, overexpression of isozyme UGT1A3 in HEK-293 cells Homo sapiens
2.4.1.17 isozyme UGT1A3, DNA and amino acid sequence determination and analysis, overexpression of isozymes UGT1A3 and UGT1A8 in HEK-293 cells Homo sapiens
2.4.1.17 overexpression of isozyme UGT1A8 in HEK-293 cells Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.004
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT2B7 Homo sapiens
2.4.1.17 0.0074
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A7 Homo sapiens
2.4.1.17 0.015
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT2B7 Homo sapiens
2.4.1.17 0.018
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT2B17 Homo sapiens
2.4.1.17 0.02
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT2B15 Homo sapiens
2.4.1.17 0.023
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A8 Homo sapiens
2.4.1.17 0.03
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A10 Homo sapiens
2.4.1.17 0.041
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT2B17 Homo sapiens
2.4.1.17 0.056
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A8 Homo sapiens
2.4.1.17 0.07
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A9 Homo sapiens
2.4.1.17 0.094
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A3 Homo sapiens
2.4.1.17 0.096
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A10 Homo sapiens
2.4.1.17 0.124
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A1 Homo sapiens
2.4.1.17 0.165
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A3 Homo sapiens
2.4.1.17 0.166
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A7 Homo sapiens
2.4.1.17 0.193
-
 cis-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A1 Homo sapiens
2.4.1.17 0.319
-
 trans-4-hydroxytamoxifen pH 7.4, 37°C, isozyme UGT1A9 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 UDP-D-glucuronate + 4-hydroxy-N-desmethyl-tamoxifen Homo sapiens the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + acceptor Homo sapiens the enzyme is involved in detoxification reactions UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + cis-4-hydroxytamoxifen Homo sapiens the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview UDP + 4-hydroxytamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + tamoxifen + H+ Homo sapiens the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview UDP + tamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + trans-4-hydroxytamoxifen Homo sapiens the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview UDP + 4-hydroxytamoxifen beta-D-glucuronoside
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens O75795 isozyme UGT2B17; isozyme UGT2B17
-
2.4.1.17 Homo sapiens P22309 isozyme UGT1A1; isozyme UGT1A1
-
2.4.1.17 Homo sapiens P22309 isozyme UGT2B7; isozyme UGT2B7
-
2.4.1.17 Homo sapiens P35503 isozyme UGT1A3; isozyme UGT1A3
-
2.4.1.17 Homo sapiens P54855 isozyme UGT2B15; isozyme UGT2B15
-
2.4.1.17 Homo sapiens Q9HAW7 isozyme UGT1A7; isozyme UGT1A7
-
2.4.1.17 Homo sapiens Q9HAW8 isozyme UGT1A10; isozyme UGT1A10
-
2.4.1.17 Homo sapiens Q9HAW9 isozyme UGT1A8; isozyme UGT1A8
-
2.4.1.17 Homo sapiens Q9HAW9 isozyme UGT1A9; isozyme UGT1A9
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
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 additional information isozyme UGT1A10 exhibits high overall glucuronidating activities compared to other UGT isozymes Homo sapiens ?
-
 ?
2.4.1.17 additional information isozyme UGT1A8 exhibits high overall glucuronidating activities compared to other UGT isozymes Homo sapiens ?
-
 ?
2.4.1.17 additional information isozyme UGT2B7 exhibits high overall glucuronidating activities compared to other UGT isozymes Homo sapiens ?
-
 ?
2.4.1.17 additional information isozymes UGT1A10, UGT1A8, and UGT2B7 exhibit the highest overall glucuronidating activities of the UGT isozymes Homo sapiens ?
-
 ?
2.4.1.17 additional information no activity by isozyme UGT2B15 with trans-4-hydroxytamoxifen Homo sapiens ?
-
 ?
2.4.1.17 UDP-D-glucuronate + 4-hydroxy-N-desmethyl-tamoxifen the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview Homo sapiens UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + 4-hydroxy-N-desmethyl-tamoxifen i.e. endoxifen, substrate synthesis, overview, O-glucuronidation by liver microsomes Homo sapiens UDP + 4-hydroxy-N-desmethyl-tamoxifen beta-D-glucuronoside product identification by HPLC and mass spectrometry analysis ?
2.4.1.17 UDP-D-glucuronate + acceptor
-
 Homo sapiens UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + acceptor the enzyme is involved in detoxification reactions Homo sapiens UDP + acceptor beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + cis-4-hydroxytamoxifen the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview Homo sapiens UDP + 4-hydroxytamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + cis-4-hydroxytamoxifen N- and O-glucuronidation by liver microsomes Homo sapiens UDP + 4-hydroxytamoxifen beta-D-glucuronoside product identification by HPLC and mass spectrometry analysis ?
2.4.1.17 UDP-D-glucuronate + tamoxifen + H+ the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview Homo sapiens UDP + tamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + tamoxifen + H+ N- and O-glucuronidation by liver microsomes Homo sapiens UDP + tamoxifen beta-D-glucuronoside product identification by HPLC and mass spectrometry analysis ?
2.4.1.17 UDP-D-glucuronate + trans-4-hydroxytamoxifen the enzyme is involved in metabolism and elimination of tamoxifen, TAM, and its major active metabolites 4-hydroxytamoxifen and 4-hydroxy-N-desmethyl-tamoxifen, i.e. endoxifen, by glucuronidation, overview Homo sapiens UDP + 4-hydroxytamoxifen beta-D-glucuronoside
-
 ?
2.4.1.17 UDP-D-glucuronate + trans-4-hydroxytamoxifen N- and O-glucuronidation by liver microsomes Homo sapiens UDP + 4-hydroxytamoxifen beta-D-glucuronoside product identification by HPLC and mass spectrometry analysis ?
2.4.1.17 UDP-D-glucuronate + trans-4-hydroxytamoxifen N- and O-glucuronidation by liver microsomes, no activity by isozyme UGT2B15 Homo sapiens UDP + 4-hydroxytamoxifen beta-D-glucuronoside product identification by HPLC and mass spectrometry analysis ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.17 UDP glucuronosyltransferase
-
 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