Glucuronide Isomers: Synthesis, Structural Characterization, and UDP-glucuronosyltransferase Screening
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چکیده
7 List of original publications 8
منابع مشابه
UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics.
Etoposide, an important anticancer agent, undergoes glucuronidation both in vitro and in vivo. In this study, three isomeric glucuronides of etoposide, including one phenolic (EPG) and two alcoholic glucuronides (EAG1 and EAG2), were biosynthesized in vitro with human liver microsomes (HLMs), and identified by liquid chromatography-electrospray ionization-mass spectrometry and confirmed by beta...
متن کاملEvidence for an UDP-glucuronic acid/phenol glucuronide antiport in rat liver microsomal vesicles.
The transport of glucuronides synthesized in the luminal compartment of the endoplasmic reticulum by UDP-glucuronosyltransferase isoenzymes was studied in rat liver microsomal vesicles. Microsomal vesicles were loaded with p-nitrophenol glucuronide (5 mM), phenolphthalein glucuronide or UDP-glucuronic acid, by a freeze-thawing method. In was shown that: (i) the loading procedure resulted in mil...
متن کاملIdentification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of posaconazole (Noxafil).
Posaconazole (Noxafil, SCH 56592), an orally available broad-spectrum triazole antifungal, is currently in phase III clinical studies for treating serious opportunistic fungal infections. The major in vitro metabolite of posaconazole formed by human liver microsomes supplemented with uridine 5'-diphosphate-glucuronic acid was a glucuronide of posaconazole (m/z877). Screening of 10 cDNA-expresse...
متن کاملThe synthesis of o-aminophenyl glucuronide in several tissues of the domestic fowl, Gallus gallus, during development.
1. Synthesis of o-aminophenyl glucuronide has been studied in tissues of the domestic fowl, Gallus gallus, during development. 2. The only route of synthesis detected is glucuronyl transfer from UDP-glucuronic acid, and evidence suggests this to be the major pathway. 3. The pathway exists in liver, to a lesser extent in kidney and alimentary tract, and possibly also in skin. It is absent from s...
متن کاملPurification and partial characterization of rat liver bilirubin glucuronoside glucuronosyltransferase.
Bilirubin glucuronoside glucuronosyltransferase (EC 2.4.1.95) converts bilirubin monoglucuronide to bilirubin diglucuronide and is concentrated in plasma membrane-enriched fractions of rat liver homogenates. The enzyme was purified 2,000-fold to homogeneity from rat liver. The pI of the enzyme is 7.9 +/- 0.2. The enzyme has a molecular weight of 160,000 and is an oligomer of 28,000 dalton subun...
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