Peptide and peptidomimetic
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Questions and Answers

What strategy can be used to increase resistance to proteolysis while retaining intended activity of peptides?

  • Using pseudo peptides
  • Replacing primary amide with secondary amides at key cleavage sites
  • Co-administering protease inhibitors and permeation enhancers
  • Replacing L-amino acids with their D-counterparts (correct)

    • Which route of administration for Leuprolide shows the highest percentage of dose absorbed?

  • Vaginal
  • Subcutaneous (correct)
  • Nasal
  • Rectal

    • What is a key advantage of using peptidomimetics in drug design?

  • Increased membrane permeation (correct)
  • Decreased bioavailability
  • Enhanced proteolysis of the drug
  • Reduced receptor binding

    • Which method is NOT a strategy to overcome the challenges posed by peptides as drug candidates?

    <p>Increasing primary amides at cleavage sites</p> Signup and view all the answers

    In nasal delivery, what aids in the effective administration of peptides?

    <p>Co-administration of protease inhibitors and permeation enhancers</p> Signup and view all the answers

    What is the main purpose of replacing non-pharmacophoric polar sections of a natural molecule with lipophilic moieties in peptidomimetics?

    <p>To increase membrane permeation</p> Signup and view all the answers

    What is the natural target for designing inhibitors of HIV protease?

    <p>S3 protease cleavage site</p> Signup and view all the answers

    Which amino acid residue in the protease mechanism forms a diol intermediate during the reaction?

    <p>Asp-25</p> Signup and view all the answers

    Which compound has the highest inhibitory potency (lowest IC50 value) among the Transition State Analogues mentioned?

    <p>CO2tBu</p> Signup and view all the answers

    What is the role of Saquinavir in peptide drug design?

    <p>Decreasing Proteolysis</p> Signup and view all the answers

    What is a key feature of Solid Phase Organic Synthesis relevant to Peptidomimetics?

    <p>Used in Combinatorial Chemistry</p> Signup and view all the answers

    How can structural extension impact the affinity of a molecule towards its target binding site?

    <p>Increasing interactions with portions of the target binding site not reached by the natural substrate</p> Signup and view all the answers

    Why is blocking the binding of fibrinogen to its receptor valuable in the treatment of stroke and heart attacks?

    <p>It prevents platelet aggregation</p> Signup and view all the answers

    What is the significance of using a Glucose scaffold analogue for a cyclic peptide agonist in inhibiting Growth Hormone (GH)?

    <p>It displays effective GH inhibition in cultured rat anterior pituitary cells</p> Signup and view all the answers

    Why are unnatural amino acids used in designing peptidomimetic drugs?

    <p>To increase affinity to target binding sites</p> Signup and view all the answers

    In peptidomimetic design, what does conformational restriction along the peptide backbone aim to achieve?

    <p>Enhance specificity and mimic secondary structures</p> Signup and view all the answers

    How does mimicking secondary structure contribute to peptidomimetic drug design?

    <p>Aids in improving the interaction with the target molecule</p> Signup and view all the answers

    What is a common way to change a peptide backbone to improve its properties?

    <p>Pseudopeptides</p> Signup and view all the answers

    How do peptidomimetics help overcome the limitations of using active peptides as drugs?

    <p>By improving hydrolytic stability and enhancing membrane penetration</p> Signup and view all the answers

    In drug discovery, what approach aims to produce hundreds to thousands of new compounds using Solid Phase Organic Synthesis?

    <p>Combinatorial approach</p> Signup and view all the answers

    What is a key advantage of peptoids in drug design?

    <p>Increased proteolysis resistance</p> Signup and view all the answers

    Why are most peptides with significant biological activity not administered unchanged as drugs?

    <p>Due to adverse ADME profiles</p> Signup and view all the answers

    Which strategy is employed by peptidomimetics to retain the activity of active peptides?

    <p>Appropriate display of binding subunits in 3-dimensional space</p> Signup and view all the answers

    Which enzymatic cleavage would be a concern for a peptide with a C-terminal residue entering the gastrointestinal tract?

    <p>Carboxypeptidases</p> Signup and view all the answers

    Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?

    <p>Their compact globular nature</p> Signup and view all the answers

    Which enzyme would be most likely to cleave a peptide at the N-terminal end?

    <p>Aminopeptidases</p> Signup and view all the answers

    In which part of the gastrointestinal tract would a peptide encounter trypsin, chymotrypsin, and elastase?

    <p>Small intestine</p> Signup and view all the answers

    Which of the following is a strategy to overcome poor passage of hydrophilic peptides through lipid membranes?

    <p>Development of peptidomimetic drugs</p> Signup and view all the answers

    Why can the enzymatic hydrolysis of peptide bonds in the gastrointestinal tract pose a challenge for oral administration of peptides?

    <p>Enzymes like pepsin and trypsin can degrade peptides</p> Signup and view all the answers

    What is the role of Saquinavir in peptide drug design?

    <p>Saquinavir acts as an HIV protease inhibitor in drug design.</p> Signup and view all the answers

    How does mimicking secondary structure contribute to peptidomimetic drug design?

    <p>Mimicking secondary structure helps enhance the stability and activity of peptidomimetics.</p> Signup and view all the answers

    What strategy can be used to increase resistance to proteolysis while retaining intended activity of peptides?

    <p>One strategy is to replace non-pharmacophoric polar sections with lipophilic moieties.</p> Signup and view all the answers

    What is the natural target for designing inhibitors of HIV protease?

    <p>The natural target is the S3 protease cleavage site in viral polypeptides.</p> Signup and view all the answers

    Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?

    <p>Full-sized proteins have more complex structures and tertiary interactions that make them less susceptible to proteolysis.</p> Signup and view all the answers

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