PHRD5915 Drug Design Lecture 14 - Drug Targets: Enzymes 2

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daynuhmay
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274182
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PHRD5915 Drug Design Lecture 14 - Drug Targets: Enzymes 2
Updated:
2014-05-15 08:16:53
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Drug Targets Enzymes
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Drug Targets: Enzymes
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  1. how is cholesterol production controlled
    by a feedback mechanism inhibiting HMGR
  2. 3 natural statins
    • 1) pravastatin
    • 2) simvastatin
    • 3) lovastatin
  3. MOA of statins
    mimic transition state of HMG-COA
  4. effect of opening the lactone ring in statins
    • improved hepatic tissue selectivity & fewer side effects
    • important for binding & ease of hydrolysis
  5. effect of added sulfonamide in statin
    generates H bonds in active site that strengthens bonding
  6. most potent statin
    rosuvastatin
  7. HIV Protease Enzyme active-site triad
    Asp25-Thr26-Gly27
  8. mimics transition state of peptide substrate of HIV-1 protease
    aspartyl warhead (on saquinavir)
  9. 2nd gen HPI
    • darunavir
    • effective against drug resistant HIV

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