PMID: 2108023Mar 10, 1990Paper

Inhibition of UDP-glucuronosyltransferase activity by possible transition-state analogues in rat-liver microsomes

European Journal of Biochemistry
D NoortG J Mulder

Abstract

A series of possible transition state analogues of the glucuronidation reaction catalyzed by UDP-glucuronosyltransferase were tested for their inhibitory effect on glucuronidation of various substrates in a rat liver microsomal fraction. In general 4-nitrophenol glucuronidation was more effectively inhibited than that of 1-naphthol, bilirubin or testosterone. 2-(1-Naphthyl)ethyl-UDP and 2,2,2-(triphenyl)ethyl-UDP were the most effective inhibitors. Their inhibitory effect was competitive towards both UDP-glucuronic acid and 4-nitrophenol. These compounds were much more effective inhibitors than UDP; therefore addition of a lipophilic group enhances the inhibitory potency of UDP. The various UDP derivatives showed differences in their abilities to inhibit the glucuronidation of the four acceptor substrates, supporting the concept that the different forms of UDP-glucuronosyl transferase have different active sites.

References

Jul 1, 1976·Analytical Biochemistry·G S RaoH Breuer
May 1, 1989·The Journal of General Physiology·B J MulderH E ter Keurs
Aug 15, 1989·European Journal of Biochemistry·S Fournel-GigleuxP Caubere
Jan 1, 1983·Pharmacology & Therapeutics·G R Stark, P A Bartlett
Sep 27, 1983·Biochemistry·P A Bartlett, C K Marlowe
Jan 1, 1981·Methods in Enzymology·B Burchell, P Weatherill

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Citations

Mar 1, 1993·Agents and Actions·R L BellG W Carter
May 14, 1999·European Journal of Drug Metabolism and Pharmacokinetics·E GolovinskyK Grancharov
Nov 1, 1995·Comparative Biochemistry and Physiology. Part C, Pharmacology, Toxicology & Endocrinology·Z NaydenovaE Golovinsky
Apr 24, 2001·Pharmacology & Therapeutics·K GrancharovE Golovinsky
Nov 17, 2001·Bioorganic & Medicinal Chemistry·P Compain, O R Martin
Nov 27, 1999·Drug Metabolism Reviews·A Radominska-PandyaP I Mackenzie
Jan 1, 1995·Critical Reviews in Toxicology·U A BoelsterliA Kretz-Rommel
Mar 1, 1992·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·P L JansenK W Bock
May 4, 2007·Journal of Medicinal Chemistry·Ingo BichlmaierJari Yli-Kauhaluoma

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