PHRD5915 Drug Design Lecture 4 - Phase II Metabolism

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daynuhmay
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266383
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PHRD5915 Drug Design Lecture 4 - Phase II Metabolism
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2014-03-14 01:55:15
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Phase II Metabolism
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Phase II Metabolism
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  1. what the MAO system does to neurotransmitters
    deamination
  2. 4 locations in which alcohol detox occurs
    • 1) microsomes
    • 2) cytosol
    • 3) peroxisomes
    • 4) mitochondria
  3. where CYP2E1 works during EtOH detox
    microsomes
  4. where ADH works during EtOH detox
    cytosol
  5. where catalase works during EtOH detox
    peroxisomes
  6. where ALD2 & ALDH1B1 work during EtOH detox
    mitochondria
  7. vitamin K analog involved in quinone cycling
    menadione
  8. how quinone-cycling causes toxicity (2)
    • 1) semiquinone radical causes protein/DNA damage
    • 2) hydroxyl radical (HO.) causes protein/DNA damage and lipid peroxidation
  9. exception to the rule that oxidative biotransformations require reduced cofactors NADPH and NADH
    peroxidases that couple the reduction of H2O2 and lipid hydroperoxides to the oxidation of other substrates => COOXIDATION
  10. 2 activities of Prostaglandin H Synthase
    • 1) cyclooxygenase
    • 2) hydroperoxidase
  11. cyclooxygenase function of Prostaglandin H Synthase in the presence of arachidonic acid
    arachidonic acid -> PGG2
  12. hydroperoxidase function of Prostaglandin H Synthase in the presence of arachidonic acid
    PGG2 -> PGH2
  13. product of PGH Synthase w/ anti-thrombotic activity
    PGH2 (prevents platelets from aggregating)
  14. how oxidative stress can be caused by xenobiotics
    take electrons from PGG2 & form free radicals

    **important in neurodegeneration**
  15. reduces free radicals formed by xenobiotics
    GSH (glutathione)
  16. what is the precursor to O-glucuronide & N+-glucuronide?
    UDP--D-glucuronic acid
  17. what transfers glucuronic acid after it is cleaved to a substrate
    uracil-glucuronic transferase (UGT)
  18. product of a glucuronidation
    glucuronide
  19. universal donor for all sulfation reations
    PAPS (3'-phosphoadenosine-5'-phosphosulfate)
  20. pyrophosphate cleavage
    2 phosphates cleaved in a rxn
  21. 3 enzymes needed for glutathione conjugation
    • 1) transpeptidase
    • 2) peptidase
    • 3) acetylase
  22. simplest of all amino acids
    glycine
  23. necessary for glycine conjugation
    Coenzyme-A  associated w/ AMP
  24. where CoA binds to carboxylic acid in glycine conjugation
    sulfur from sulfhydryl group
  25. needed for glycine conjugation (3)
    • 1) acyl-CoA synthase (replaces -OH w/ AMP, then CoASH)
    • 2) CoA (activates carboxyl group, then is leaving group)
    • 3) N-acyltransferase (takes off CoA)
  26. thiol metabolism
    thiol -> disulfide

    (by oxidation)
  27. enzyme that cleaves disulfide bond
    glutathione reductase
  28. enzyme that oxidizes a substrate
    P450 (monooxygenase)
  29. requirement for conjugation
    drug/molecule has to be hydroxylated first
  30. leaving groups in glucuronidation
    • phosphate groups
    • uracil
  31. substrates you can conjugate glucuronic acid to3
    • ROH
    • R3N

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