Question

sdent ork 10/27/17 50% 1st attempt Structure-based drug design strategies often devise competitive Inhibitors that bind to certain enzyme active sites. For example saquinavir and Indinavir are designed HIV protease inhibitors that bind to the aspartate protease enzyme of HIV, which is required for the virus to produce functional proteins for further HIV infection. Which of the following statements are true about saquinavir and Indinavir? Choose one or more: A. Very high local concentrations of proteins with Phe-Pro or Tyr-Pro peptide bonds would reduce the B. The removal of the phenyi ring (six-membered carbon ring containing three double bonds and no attached C. Increasing concentrations of indinavir or saquinavir would result in a change in the a of the aspartate D. Saquinav effectiveness of saquinavir and indinavir in limiting HiV's infectivity of new cells. functional groups) on indinavir and saquinavir would likely affect their Inhibitory activity protease enzyme reaction vir and indinavir both have a component that mimics the natural Phe-Pro dipeptide substrate of aspartate protease 17,30

Answer 1

HIV protease inhibitors are peptide-like chemicals that competitively inhibit the action of the virus aspartyl protease. A peptide linkage consisting of –NH-CO- is replaced by an hydroxyethylen group (-CH₂-CH(OH)-) which the protease is unable to cleave. HIV-1 protease cleaves the sequences containing the dipeptides Tyr-Pro or Phe-Pro was the basic design criterion. Indinavir is Phe-Gly. The terminal phenyl constituents contribute hydrophobic binding to increase potency. HIV inhibitors change Vo but not Vmax.

1st attempt O See Hi Structure-based drug design strategies often devise competizive inhibitors that bind to certain enzyme active sites For example saquinavir and Indinavir are designed HIV protease inhibitors that bind to the aspartate protease enzyme of HIV which is required for the virus to produce functional proteins for further HIV infection. Which of the following statements are true about saquinavir and Indinavir? Choose one or more: A Verv high local concentrations of proteins with Phe-Pro or Tyr-Prop effectiveness of saqulnavir and indinavir in limiting HIV's infectivity of new celts The removal functional groupsi on indinavir and saquinavir would tikely affect their inhibitory activity of the phenylring (six-membered carbon ring containing three double bonds and no attached Squinavir and indinavir both have a component hot spartate protease

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