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Literature summary extracted from

  • Cheng, Z.; Rios, G.R.; King, C.D.; Coffman, B.L.; Green, M.D.; Mojarrabi, B.; Mackenzie, P.I.; Tephly, T.R.
    Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7 (1998), Toxicol. Sci., 45, 52-57.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.17 expressed in HK293 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.17 2-hydroxyestradiol inhibits 4-hydroxyestradiol glucuronidation catalyzed by UGT2B7Y Homo sapiens
2.4.1.17 4-hydroxyestradiol inhibits 2-hydroxyestradiol glucuronidation catalyzed by UGT1A1 Homo sapiens
2.4.1.17 flunitrazepam competitive inhibition of estrogen and buprenorphine catalyzed by UGT1A1 and UGT2B7Y, not inhibition of UGT1A3 Homo sapiens
2.4.1.17 additional information norepinephrine does not inhibit UGT2B7Y, UGT1A1 nor UGT1A3 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.1.17 0.006
-
 4-hydroxyestradiol apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.007
-
 4-hydroxyestradiol apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.014
-
 2-hydroxyestradiol apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.016
-
 4-hydroxyestrone apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.019
-
 4-hydroxyestrone apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.024
-
 2-hydroxyestrone apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.026
-
 2-hydroxyestrone apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.026
-
 2-hydroxyestradiol apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.027
-
 2-hydroxyestradiol apparent Km on expressed UGT1A1, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.038
-
 4-hydroxyestradiol apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.053
-
 4-hydroxyestrone apparent Km on expressed UGT1A3, 2 mM UDP glucuronic acid Homo sapiens
2.4.1.17 0.066
-
 2-hydroxyestrone apparent Km on expressed UGT2B7Y, 2 mM UDP glucuronic acid Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.4.1.17 nuclear membrane
-
 Homo sapiens 31965
-

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.17 Homo sapiens
-
-
-

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 2-hydroxyestradiol + UDPglucuronate
-
 Homo sapiens UDP + 2-hydroxyestradiol O-glucuronide
-
 ?
2.4.1.17 2-hydroxyestrone + UDPglucuronate
-
 Homo sapiens 2-hydroxyestrone 2-O-glucuronide + UDP
-
 ?
2.4.1.17 4-hydroxyestradiol + UDPglucuronate
-
 Homo sapiens UDP + 4-hydroxyestradiol O-glucuronide
-
 ?
2.4.1.17 4-hydroxyestrone + UDP-glucuronate
-
 Homo sapiens UDP + 4-hydroxyestrone 4-O-glucuronide
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.1.17 0.022
-
 flunitrazepam inhibition of 2-hydroxyestrone glucuronidation catalyzed by UGT1A3 Homo sapiens
2.4.1.17 0.03
-
 flunitrazepam inhibition of 2-hydroxyestradiol glucuronidation catalyzed by UGT1A3 Homo sapiens
2.4.1.17 0.047
-
 flunitrazepam inhibition of nalorphine glucuronidation catalyzed by UGT2B7Y Homo sapiens
2.4.1.17 0.052
-
 flunitrazepam inhibition of 4-hydroxyestrone glucuronidation catalyzed by UGT2B7Y Homo sapiens
2.4.1.17 0.061
-
 flunitrazepam inhibition of 4-hydroxyestradiol glucuronidation catalyzed by UGT2B7Y Homo sapiens
2.4.1.17 0.093
-
 flunitrazepam inhibition of buprenorphine glucuronidation catalyzed by UGT2B7Y Homo sapiens
2.4.1.17 0.206
-
 flunitrazepam inhibition of buprenorphine glucuronidation catalyzed by UGT1A1 Homo sapiens
2.4.1.17 0.402
-
 flunitrazepam inhibition of 2-hydroxyestradiol glucuronidation catalyzed by UGT1A1 Homo sapiens
2.4.1.17 0.808
-
 flunitrazepam inhibition of 2-hydroxyestrone glucuronidation catalyzed by UGT1A1 Homo sapiens