lect 8 ___ Lecture 7 Phase II UGT

lect 8 ___ Lecture 7 Phase II UGT - NS120/220...

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1 NS120/220 Glucuronidation and UGTs O O OH COO - P O O P O CH 2 O HN N O O O Learning Objectives Define Phase II reactions. Describe the high energy co-factor in glucoronidation and explain their role in biotransformation reactions. Describe the reaction mechanisms of Glucuronidation. Explain how you could determine the substrate specificity of UGTs. Describe the three diseases of unconjugated hyperbilirudinemia and what kinds of mutations cause these diseases.
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2 Readings HUMAN UDP-GLUCURONOSYLTRANSFERASES : Metabolism, Expression, and Disease, Annu. Rev. Pharmacol. Toxicol. 2000. 40:581–616 General Scheme of Xenobiotic Xenobiotic Metabolism Lipophilic Hydrophilic Metabolism Increase excretability Decrease biological activity Phase I (oxidative) Parent compound Metabolites polarity functionality Phase II (synthetic) Metabolites size ionization water solubility
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3 Phase II Enzyme Reactions O OP O O - O O - OC H 2 OH OH COO- HO O OH OH N NH O O G l u c u r o n i d a t i o n Enzyme: Glucuronosyltransferases (UGT) cofactor: uridine-5'-diphospho-D-glucuronic acid (UDP-GA) S O O - O O O - H 2 O OO H PO 3 2- N N N N H 2 N S u l f a t i o n Enzyme: Sulfotransferases (ST)
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lect 8 ___ Lecture 7 Phase II UGT - NS120/220...

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