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Literature summary for 2.4.1.17 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
Search for more literature for 2.4.1.17

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HK293 cells Homo sapiens

Inhibitors

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

KM Value [mM]

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

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-hydroxyestradiol + UDPglucuronate
-
 Homo sapiens UDP + 2-hydroxyestradiol O-glucuronide
-
 ?
2-hydroxyestrone + UDPglucuronate
-
 Homo sapiens 2-hydroxyestrone 2-O-glucuronide + UDP
-
 ?
4-hydroxyestradiol + UDPglucuronate
-
 Homo sapiens UDP + 4-hydroxyestradiol O-glucuronide
-
 ?
4-hydroxyestrone + UDP-glucuronate
-
 Homo sapiens UDP + 4-hydroxyestrone 4-O-glucuronide
-
 ?

Ki Value [mM]

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