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Questions and Answers
What plays a crucial role in the formation of GSH conjugates of electrophilic xenobiotics or metabolites?
What plays a crucial role in the formation of GSH conjugates of electrophilic xenobiotics or metabolites?
- Xenobiotic metabolizing enzymes
- Electrophilic enzymes
- Mercapturic acid enzymes
- GSH S-transferases (correct)
What is the product of the conjugation reaction between GSH and electrophilic xenobiotics or metabolites?
What is the product of the conjugation reaction between GSH and electrophilic xenobiotics or metabolites?
- GSH conjugates
- Xenobiotic metabolites
- Electrophilic acids
- Mercapturic acids (correct)
What type of xenobiotics or metabolites undergo conjugation with GSH?
What type of xenobiotics or metabolites undergo conjugation with GSH?
- Inactive
- Nucleophilic
- Reactive
- Electrophilic (correct)
What is the role of GSH S-transferases in the conjugation reaction?
What is the role of GSH S-transferases in the conjugation reaction?
What is the result of the conversion of GSH conjugates of electrophilic xenobiotics or metabolites?
What is the result of the conversion of GSH conjugates of electrophilic xenobiotics or metabolites?
Which of the following compounds is not a primary amino group, but can still undergo acetylation?
Which of the following compounds is not a primary amino group, but can still undergo acetylation?
What is the functional group that undergoes acetylation in primary aromatic amines?
What is the functional group that undergoes acetylation in primary aromatic amines?
Which of the following statements is true about the acetylation of hydrazines?
Which of the following statements is true about the acetylation of hydrazines?
What is the general term for the functional group that undergoes acetylation in sulfonamides?
What is the general term for the functional group that undergoes acetylation in sulfonamides?
Which of the following compounds can undergo acetylation due to the presence of a primary amino group?
Which of the following compounds can undergo acetylation due to the presence of a primary amino group?
What is the primary functional group that undergoes sulfation in sulfate conjugation?
What is the primary functional group that undergoes sulfation in sulfate conjugation?
Which of the following compounds is NOT a common substrate for sulfation?
Which of the following compounds is NOT a common substrate for sulfation?
What is the primary step in the sulfate conjugation process?
What is the primary step in the sulfate conjugation process?
Which of the following is the order of preference for sulfation?
Which of the following is the order of preference for sulfation?
Which of the following is a characteristic of sulfate conjugation?
Which of the following is a characteristic of sulfate conjugation?
What is the role of PAPS in sulfate conjugation?
What is the role of PAPS in sulfate conjugation?
What is the result of the process involving γ-glutamylcysteine}
What is the result of the process involving γ-glutamylcysteine}
What is the product of the reaction involving glutathione?
What is the product of the reaction involving glutathione?
What is the outcome of the enzymatic cleavage of two amino acids?
What is the outcome of the enzymatic cleavage of two amino acids?
What is the purpose of N-acetylation in this process?
What is the purpose of N-acetylation in this process?
What is the intermediate formed in the process involving γ-glutamylcysteine?
What is the intermediate formed in the process involving γ-glutamylcysteine?
What is the final product of the process involving γ-glutamylcysteine?
What is the final product of the process involving γ-glutamylcysteine?
What is the result of regioselective O-demethylation of the 4-OCH3 group in papaverine?
What is the result of regioselective O-demethylation of the 4-OCH3 group in papaverine?
What has changed significantly in recent years regarding drug metabolites?
What has changed significantly in recent years regarding drug metabolites?
What is the current understanding of pharmacologically active metabolites?
What is the current understanding of pharmacologically active metabolites?
What is the name of the process by which the 4-OCH3 group in papaverine is converted to an alcohol?
What is the name of the process by which the 4-OCH3 group in papaverine is converted to an alcohol?
What is the significance of pharmacologically active metabolites in drug therapy?
What is the significance of pharmacologically active metabolites in drug therapy?
What is the implication of increasing evidence on pharmacologically active metabolites?
What is the implication of increasing evidence on pharmacologically active metabolites?
Study Notes
Sulfate Conjugation
- Sulfate conjugation (sulfation) is less frequent compared to glucuronide conjugation (glucuronidation)
- The most common functional groups that undergo sulfation are free OH, NH2, and NHOH
- Phenols (Ph-OH) are the main group of substrates that undergo sulfate conjugation, followed by:
- Alcohols (ROH)
- Aromatic amines (ph-NH)
- N-hydroxyl (N-OH)
Substrates of Sulfate Conjugation
- Sulfation is used to conjugate endogenous compounds, including:
- Steroids
- Heparin
- Chondroitin
- Catecholamines
- Thyroxine
Sulfate Conjugation Process
- The process involves the activation of inorganic sulfate (SO4) to form CoEnzyme 3′-phosphoadenosine-5′-phosphosulfate (PAPS)
GSH Conjugation
- Formation of GSH conjugates of electrophilic xenobiotics or metabolites (E) occurs through enzymatic cleavage of two amino acids (glutamic acid and glycine) from the formed GSH adduct
- Subsequent N-acetylation of the remaining S-substituted cysteine residue forms mercapturic acids
- Conjugation of substrates with GSH is catalyzed by enzymes known as GSH S-transferases
Acetylation
- The functional group undergoing acetylation is the primary amino group (NH2), including:
- Primary aromatic amines (ArNH2)
- Sulfonamides (H2NC6H4SO2NHR)
- Hydrazines (-NHNH2)
Pharmacologically Active Metabolites
- The traditional idea that drug metabolites are inactive and insignificant in drug therapy has changed dramatically in recent years
- Evidence suggests that many drugs undergo biological transformation, leading to pharmacologically active metabolites
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Description
Learn about sulfate conjugation, a type of phase II biotransformation, its frequency, and the most common functional groups that undergo sulfation, including phenols and alcohols.
