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Molecular Pharmacology

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Abstract

Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol.

T Ebner, R P Remmel and B Burchell
Molecular Pharmacology April 1993, 43 (4) 649-654;
T Ebner
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R P Remmel
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B Burchell
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Abstract

The synthetic estrogen ethinylestradiol is extensively eliminated as glucuronide metabolites in humans, but the UDP-glucuronosyltransferases (UGTs) catalyzing this reaction have not been identified. Therefore, ethinylestradiol was tested as a substrate for cloned human UGTs stably expressed in V79 cell lines. Two cloned expressed human enzymes, a bilirubin UGT and a phenol UGT, were observed to catalyze the glucuronidation of ethinylestradiol. High performance liquid chromatographic analysis of the products formed revealed that the expressed bilirubin UGT specifically produced ethinylestradiol-3-glucuronide. In human liver microsomes the ratio of 3-glucuronide/17-glucuronide was 97:3. Subsequent study of the cloned expressed enzymes and human liver microsomes from Crigler-Najjar patients by kinetic analysis and by substrate inhibition strongly indicated that a human liver bilirubin UGT was largely responsible for glucuronidation of ethinylestradiol. These results may provide an explanation for jaundice caused by ethinylestradiol in certain susceptible individuals.

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Molecular Pharmacology
Vol. 43, Issue 4
1 Apr 1993
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Abstract

Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol.

T Ebner, R P Remmel and B Burchell
Molecular Pharmacology April 1, 1993, 43 (4) 649-654;

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Abstract

Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol.

T Ebner, R P Remmel and B Burchell
Molecular Pharmacology April 1, 1993, 43 (4) 649-654;
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