Title : Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7.

Pub. Date : 1998 Sep

PMID : 9848110






7 Functional Relationships(s)
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1 Three human liver UDP-glucuronosyltransferases, UGT2B7, UGT1A1, and UGT1A3, have been shown to catalyze the glucuronidation of catechol estrogens and lead to their enhanced elimination via urine or bile. catechol UDP glucuronosyltransferase family 2 member B7 Homo sapiens
2 UGT2B7(Y) reacted with higher efficiency toward 4-hydroxyestrogenic catechols, whereas UGT1A1 and UGT1A3 showed higher activities toward 2-hydroxyestrogens. Catechols UDP glucuronosyltransferase family 2 member B7 Homo sapiens
3 UGT2B7(H) catalyzed estrogen catechol glucuronidation with efficiencies similar to UGT2B7(Y). catechol UDP glucuronosyltransferase family 2 member B7 Homo sapiens
4 Flunitrazepam (FNZ), a competitive inhibitor of morphine glucuronidation in hepatic microsomes, competitively inhibited catechol estrogen glucuronidation catalyzed by UGT2B7(Y), UGT1A1, and UGT1A3. Flunitrazepam UDP glucuronosyltransferase family 2 member B7 Homo sapiens
5 Flunitrazepam (FNZ), a competitive inhibitor of morphine glucuronidation in hepatic microsomes, competitively inhibited catechol estrogen glucuronidation catalyzed by UGT2B7(Y), UGT1A1, and UGT1A3. Morphine UDP glucuronosyltransferase family 2 member B7 Homo sapiens
6 Flunitrazepam (FNZ), a competitive inhibitor of morphine glucuronidation in hepatic microsomes, competitively inhibited catechol estrogen glucuronidation catalyzed by UGT2B7(Y), UGT1A1, and UGT1A3. catechol UDP glucuronosyltransferase family 2 member B7 Homo sapiens
7 FNZ competitively inhibited buprenorphine glucuronidation with UGT1A1 and UGT2B7 but had no inhibitory activity toward UGT1A3. Buprenorphine UDP glucuronosyltransferase family 2 member B7 Homo sapiens