Title : Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of posaconazole (Noxafil).

Pub. Date : 2004 Feb

PMID : 14744950






4 Functional Relationships(s)
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1 Screening of 10 cDNA-expressed recombinant human UDP-glucuronosyltransferase (UGT) enzymes showed that only UGT1A4 exhibited catalytic activity with respect to the formation of the glucuronide of posaconazole. Glucuronides UDP glucuronosyltransferase family 1 member A4 Homo sapiens
2 The formation of glucuronide by human liver microsomes and UGT1A4 was inhibited by bilirubin, a known inhibitor of UGT1A4. Glucuronides UDP glucuronosyltransferase family 1 member A4 Homo sapiens
3 The formation of glucuronide by human liver microsomes and UGT1A4 was inhibited by bilirubin, a known inhibitor of UGT1A4. Glucuronides UDP glucuronosyltransferase family 1 member A4 Homo sapiens
4 There was a high correlation (r =0.90) between the rate of formation of glucuronide, determined in 10 human liver microsomal samples, and trifluoperazine glucuronidation catalyzed by UGT1A4. Glucuronides UDP glucuronosyltransferase family 1 member A4 Homo sapiens