UDP-glucuronosyl transferases + glucuronidation

• What percentage is mentioned in the study material?

  10%
• What year is referenced in the study material?

  2005
• What does CV4 COP-Glucuronary refer to?

  It refers to tranverates and glucuronidation.
• What are phase 2 metabolites associated with?

  They are associated with glucuronidation processes.
• What is the purpose of glucuronidation in drug metabolism?

  It allows for the excretion of drugs or metabolites by making them more water-soluble.
• What type of group is added during glucuronidation?

  A water-soluble group.
• What types of conjugation are included in glucuronidation?

  Glucuronidation, sulfonation, and glutathione conjugation.
• What are some conjugation processes mentioned in the study material?

  Phosphorylation, methylation, acetylation, and acylation.
• What is the role of CoA in metabolism?

  It is involved in the metabolism of fatty acids and carbohydrates.
• What is the key process highlighted in the study material?

  Glucuronidation.
• What is added during glucuronidation?

  Glucuronic acid is added to nucleophiles.
• What must nucleophiles possess for glucuronidation to occur?

  Nucleophiles must possess lone pairs and a negative charge.
• What are some examples of common nucleophiles?


  Phenols, carboxylates, and amines.
• What is mentioned as a type of nucleophile in the study material?

  Phenols.
• What is UDPGT an abbreviation for?

  UDP-glucuronic acid transferase.
• What is the most common reaction in phase 2 metabolism?

  Glucuronidation.
• What happens to the configuration of compounds during glucuronidation?

  They undergo inversion of configuration.
• What is the variable amount that can be glucuronidated?

  It can range from approximately 11 to 9000.
• What is the structure of UDPGT described as?

  A quaternary protein structure.
• Where is UDPGT found in the body?

  It is found in the endoplasmic reticulum membrane.
• In which tissues is UDPGT predominantly found?

  It is found in the liver, skin, intestine, kidney, and adrenal glands.
• What is the molecular weight of UDPGT mentioned in the study material?

  Approximately 20,000 Da.
• How does UDPGT expression differ in babies compared to adults?

  Babies have low expression and enzyme activity, leading to extended elimination times.
• How does age affect UDPGT metabolism in dogs?

  Elderly dogs have 2-3 times more metabolism than younger dogs.
• What is the significance of enterohepatic circulation?

  It salvages important compounds like steroid hormones.
• How does glucuronidation affect the apparent half-life of a drug?

  It increases the apparent half-life due to drug reabsorption.
• What is the classification of the UDPGT super-family based on molecular weight?

  Enzymes have a molecular weight of 10-60 kDa.
• Which UDPGT enzymes are important in drug metabolism?

  1A1, 1A2, 1A4, 1A6, 2B4, 2B7, 2B10, 2B11, 2B15.
• What causes variations in UDPGTs?

  Variations are caused by polymorphisms affecting drug metabolism.
• What is Gilbert's Syndrome associated with?

  It is associated with a common UDPGT deficiency.
• What is the biochemical consequence of Gilbert's Syndrome?

  It leads to elevated levels of bilirubin due to impaired glucuronidation.
• What is the most common mutation in Caucasians related to UDPGT?

  It is a defect in the promoter of UDPGT1A1.
• What is the consequence of mutations in UDPGT expression?

  They can lead to variations in drug metabolism and toxicity.
• What factors can trigger cyclical jaundice in individuals?

  Factors include heavy exercise, dehydration, and stress.
• What can occur due to UDPGT deficiencies?

  It can lead to increased levels of drugs in the bloodstream.
• How can drug metabolism be influenced by environmental factors?

  Environmental factors like cigarette smoke and pollutants can induce metabolism.
• What determines which compounds get glucuronidated?

  It depends on the nucleophilicity of the groups available.
• What can UDPGT produce that has pharmacological significance?

  It can produce various metabolites with different pharmacological activities.