Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes

Basic and Clinical Pharmacology and Toxicology

Volumn 101, Issue 3, 2007, Pages 211-214

  Mano, Yuji ^a   Usui, Takashi ^a   Kamimura, Hidetaka ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ESTRADIOL; ESTRADIOL 3BETA GLUCURONIDE; ETHINYLESTRADIOL; GLUCURONOSYLTRANSFERASE 1A1; HYMECROMONE; PROPOFOL; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG MECHANISM; ENZYME ACTIVATION; ENZYME ACTIVITY; GLUCURONIDATION; HUMAN; HUMAN TISSUE; LIVER MICROSOME; MICHAELIS MENTEN KINETICS; MODULATION; PRIORITY JOURNAL;

ESTRADIOL; ETHINYL ESTRADIOL; GLUCURONIDES; GLUCURONOSYLTRANSFERASE; HUMANS; HYMECROMONE; MICROSOMES, LIVER; PROPOFOL; RECOMBINANT PROTEINS;

EID: 34547869210     PISSN: 17427835     EISSN: 17427843     Source Type: Journal    
DOI: 10.1111/j.1742-7843.2007.00112.x     Document Type: Article

References (16)

1. Bosma PJ, Seppen J, Goldhoom B et al. Bilirubin UDP- glucuronosyltransferase 1 is the only relevant bilirubin glucuronidating isoform in man. J Biol Chem 1994 269 : 17960 4.
2. Senafi SB, Clarke DJ, Burchell B. Investigation of the substrate specificity of a cloned expressed human bilirubin UDP-glucuronosyltransferase: UDP-sugar specificity and involvement in steroid and xenobiotic glucuronidation. Biochem J 1994 303 : 233 40.
3. Hanioka N, Ozawa S, Jinno H, Ando M, Saito Y, Sawada J. Human liver UDP-glucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin. Xenobiotica 2001 31 : 687 99.
4. Kiang TK, Ensom MH, Chang TK. UDP-glucuronosyltransferases and clinical drug-drug interactions. Pharmacol Ther 2005 106 : 97 132.
5. Mano Y, Usui T, Kamimura H. Effects of β-estradiol and propofol on the 4-methylumbelliferone glucuronidation in recombinant human UGT isozymes 1A1, 1A8 and 1A9. Biopharm Drug Dispos 2004 25 : 339 44.
6. Williams JA, Ring BJ, Cantrell VE et al. Differential modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1)-catalyzed estradiol-3-glucuronidation by the addition of UGT1A1 substrates and other compounds to human liver microsomes. Drug Metab Dispos 2002 30 : 1266 73.
7. Pfeiffer E, Treiling CR, Hoehle SI, Metzler M. Isoflavones modulate the glucuronidation of estradiol in human liver microsomes. Carcinogenesis 2005 26 : 2172 8.
8. Mano Y, Usui T, Kamimura H. In vitro inhibitory effects of non-steroidal antiinflammatory drugs on UDP-glucuronosyltransferase 1A1-catalysed estradiol 3β-glucuronidation in human liver microsomes. Biopharm Drug Dispos 2005 26 : 35 9.
9. Uchaipichat V, Mackenzie PI, Guo XH et al. Human UDP- glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab Dispos 2004 32 : 413 23.
10. Mano Y, Usui T, Kamimura H. Comparison of inhibition potentials of drugs against zidovudine glucuronidation in rat hepatocytes and liver microsomes. Drug Metab Dispos 2007 35 : 602 6.
11. Sorich MJ, Smith PA, McKinnon RA, Miners JO. Pharmacophore and quantitative structure activity relationship modelling of UDP- glucuronosyltransferase 1A1 (UGT1A1) substrates. Pharmacogenetics 2002 12 : 635 45.
12. Ngui JS, Tang W, Stearns RA et al. Cytochrome P450 3A4-mediated interaction of diclofenac and quinidine. Drug Metab Dispos 2000 28 : 1043 50.
13. Schrag ML, Wienkers LC. Covalent alteration of the CYP3A4 active site: evidence for multiple substrate binding domains. Arch Biochem Biophys 2001 391 : 49 55.
14. Ghosh SS, Sappal BS, Kalpana GV, Lee SW, Chowdhury JR, Chowdhury NR. Homodimerization of human bilirubin-uridine-diphosphoglucuronate glucuronosyltransferase-1 (UGT1A1) and its functional implications. J Biol Chem 2001 276 : 42108 15.
15. Hagenauer B, Salamon A, Thalhammerm T et al. In vitro glucuronidation of the cyclin-dependent kinase inhibitor flavopiridol by rat and human liver microsomes: involvement of UDP-glucuronosyltransferases 1A1 and 1A9. Drug Metab Dispos 2001 29 : 407 14.
16. Soars MG, Burchell B, Riley RJ. In vitro analysis of human drug glucuronidation and prediction of in vivo metabolic clearance. J Pharmacol Exp Ther 2002 301 : 382 90.