PHRD5915 Drug Design Lecture 13 - Drug Targets: Enzymes 1

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PHRD5915 Drug Design Lecture 13 - Drug Targets: Enzymes 1
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2014-05-12 14:33:27
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Drug Targets Enzymes
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Drug Targets: Enzymes 1
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  1. enzyme catalyst MOA
    reduce activation energy required, increasing rate of reaction
  2. constant & theoretical maximal rate of the reaction
    Vmax
  3. small Km =
    tight binding
  4. high Km =
    weak binding
  5. under true M-M conditions, it is an estimate of the dissociation constant of E from S
    Km
  6. inhibitors that interact w/ an enzyme via noncovalent associations
    reversible inhibitors
  7. inhibitors that interact w/ an enzyme via covalent associations
    irreversible inhibitors
  8. 2 types of reversible inhibitors
    • competitive
    • noncompetitive
  9. inhibitor that binds only to E (NOT to ES)
    competitive
  10. inhibitor that binds either to E and/or to ES
    noncompetitive
  11. inhibitor that results in same Vmax, increased Km
    competitive inhibitor
  12. inhibitor that results in same Km, decreased Vmax
    noncompetitive
  13. inhibitors that bind reversibly to the active site
    competitive
  14. inhibitors that bind to other parts of the enzyme, distorting its shape & active site
    noncompetitive
  15. noncompetitive inhibitor ____ (can/cannot) be overcome by increasing [S].
    cannot
  16. competitive inhibitor _____ (can/cannot) be overcome by increasing [S]
    can
  17. difference between mixed inhibition & noncompetitive
    EIS (enzyme inhibitor substrate) complex has residual enzymatic activity in mixed inhibition
  18. inhibition that results in reduced Vmax and inc OR dec Km
    mixed inhibition
  19. inhibition where inhibitor binds only to the enzyme substrate complex
    incompetitive
  20. inhibition resulting in decreased Vmax AND Km by the same amount
    uncompetitive
  21. example of irreversibly enzyme inhibitor
    serine protease inhibitors
  22. serine protease that is a potent inhibitor of bacterial -lactamase
    clavulanic acid
  23. principle enzyme responsible for penicillin-resistant bacteria
    clavulanic acid
  24. MOA of Michael acceptor against -lactamase
    alkylates nucleophilic residue on -lactamase, causing irreversible inhibition
  25. natural agonist of muscarinic-R's
    muscarine
  26. natural antagonist of muscarinic-R's
    atropine
  27. reversible AChE inhibitor from the African Calabar Bean
    physostigmine
  28. what is physostigmine used to treat?
    • myasthenia gravis
    • glaucoma
    • Alzheimer's disease
    • delayed gastric emptying
  29. site on AChE alkylated by Sarin
    esteratic site
  30. how did pyridostigmine cause the Gulf War Syndrome?
    under high stress (eg: at war), the BBB becomes leaky => pyridostigmine was able to get into the CNS & cause SE's
  31. targeted anticancer drugs
    tyrosine kinase inhibitors
  32. Philadelphia Chromosome in CML
    BCR-ABL fusion protein
  33. 4 steps for dev of imatinib
    • 1) pyrimidine ring added to activate
    • 2) amide for activity against BCR-ABL
    • 3) methyl group to eliminate PKC activity
    • 4) R1 changed to ring to inc water solubility/bioavailability
  34. binds to inactive ABL
    imatinib
  35. binds to active ABL
    dasatinib
  36. molecular target of clavulanic acid
    -lactamase
  37. molecular target of neostigmine
    reversible inhibitor of AChE
  38. molecular target of nerve gas agents (Sarin, Tabun, DFP, VX)
    irreversible AChE inhibitors
  39. muscarine treats
    glaucoma
  40. atropine treats
    organophosphate poisoning & resuscitation
  41. neostigmine treats
    myasthenia gravis (autoimmune)
  42. molecular target of pralidoxime
    removes irreversible organophosphate inhibitors from AChE
  43. molecular target of pyridostigmine
    prophylatic to block/prevent organophosphate binding to AChE
  44. molecular target of imatinib (Gleevec)
    competitive BCR-ABL inhibitor binds to inactive ABL
  45. molecular target of dasatinib (Sprycel)
    binds to active form of ABL

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