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The effect of valproic acid on drug and steroid glucuronidation by expressed human UDP-glucuronosyltransferases

✍ Scribed by Brian T Ethell; Gail D Anderson; Brian Burchell


Book ID
113993448
Publisher
Elsevier Science
Year
2003
Tongue
English
Weight
187 KB
Volume
65
Category
Article
ISSN
0006-2952

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The effect of valproic acid on drug and
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Valproic acid glucuronidation kinetics were carried our with three human UGT isoforms: UGT1A6, UGT1A9, and UGT2B7 as well as human liver and kidney microsomes. The glucuronidation of valproic acid was typified by high K(m) values with microsomes and expressed UGTs (2.3-5.2mM). The ability of valproi

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The inhibitory potencies of non-steroidal anti-inflammatory drugs (NSAIDs) on UDP-glucuronosyltransferase (UGT) 1A9 activity were investigated in recombinant human UGT1A9 using 4-methylumbelliferone (4-MU) as a substrate for glucuronidation. 4-MU glucuronidation (4-MUG) showed Michaelis-Menten kinet