Podcast
Questions and Answers
What strategy can be used to increase resistance to proteolysis while retaining intended activity of peptides?
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?
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?
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?
Which method is NOT a strategy to overcome the challenges posed by peptides as drug candidates?
In nasal delivery, what aids in the effective administration of peptides?
In nasal delivery, what aids in the effective administration of peptides?
What is the main purpose of replacing non-pharmacophoric polar sections of a natural molecule with lipophilic moieties in peptidomimetics?
What is the main purpose of replacing non-pharmacophoric polar sections of a natural molecule with lipophilic moieties in peptidomimetics?
What is the natural target for designing inhibitors of HIV protease?
What is the natural target for designing inhibitors of HIV protease?
Which amino acid residue in the protease mechanism forms a diol intermediate during the reaction?
Which amino acid residue in the protease mechanism forms a diol intermediate during the reaction?
Which compound has the highest inhibitory potency (lowest IC50 value) among the Transition State Analogues mentioned?
Which compound has the highest inhibitory potency (lowest IC50 value) among the Transition State Analogues mentioned?
What is the role of Saquinavir in peptide drug design?
What is the role of Saquinavir in peptide drug design?
What is a key feature of Solid Phase Organic Synthesis relevant to Peptidomimetics?
What is a key feature of Solid Phase Organic Synthesis relevant to Peptidomimetics?
How can structural extension impact the affinity of a molecule towards its target binding site?
How can structural extension impact the affinity of a molecule towards its target binding site?
Why is blocking the binding of fibrinogen to its receptor valuable in the treatment of stroke and heart attacks?
Why is blocking the binding of fibrinogen to its receptor valuable in the treatment of stroke and heart attacks?
What is the significance of using a Glucose scaffold analogue for a cyclic peptide agonist in inhibiting Growth Hormone (GH)?
What is the significance of using a Glucose scaffold analogue for a cyclic peptide agonist in inhibiting Growth Hormone (GH)?
Why are unnatural amino acids used in designing peptidomimetic drugs?
Why are unnatural amino acids used in designing peptidomimetic drugs?
In peptidomimetic design, what does conformational restriction along the peptide backbone aim to achieve?
In peptidomimetic design, what does conformational restriction along the peptide backbone aim to achieve?
How does mimicking secondary structure contribute to peptidomimetic drug design?
How does mimicking secondary structure contribute to peptidomimetic drug design?
What is a common way to change a peptide backbone to improve its properties?
What is a common way to change a peptide backbone to improve its properties?
How do peptidomimetics help overcome the limitations of using active peptides as drugs?
How do peptidomimetics help overcome the limitations of using active peptides as drugs?
In drug discovery, what approach aims to produce hundreds to thousands of new compounds using Solid Phase Organic Synthesis?
In drug discovery, what approach aims to produce hundreds to thousands of new compounds using Solid Phase Organic Synthesis?
What is a key advantage of peptoids in drug design?
What is a key advantage of peptoids in drug design?
Why are most peptides with significant biological activity not administered unchanged as drugs?
Why are most peptides with significant biological activity not administered unchanged as drugs?
Which strategy is employed by peptidomimetics to retain the activity of active peptides?
Which strategy is employed by peptidomimetics to retain the activity of active peptides?
Which enzymatic cleavage would be a concern for a peptide with a C-terminal residue entering the gastrointestinal tract?
Which enzymatic cleavage would be a concern for a peptide with a C-terminal residue entering the gastrointestinal tract?
Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?
Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?
Which enzyme would be most likely to cleave a peptide at the N-terminal end?
Which enzyme would be most likely to cleave a peptide at the N-terminal end?
In which part of the gastrointestinal tract would a peptide encounter trypsin, chymotrypsin, and elastase?
In which part of the gastrointestinal tract would a peptide encounter trypsin, chymotrypsin, and elastase?
Which of the following is a strategy to overcome poor passage of hydrophilic peptides through lipid membranes?
Which of the following is a strategy to overcome poor passage of hydrophilic peptides through lipid membranes?
Why can the enzymatic hydrolysis of peptide bonds in the gastrointestinal tract pose a challenge for oral administration of peptides?
Why can the enzymatic hydrolysis of peptide bonds in the gastrointestinal tract pose a challenge for oral administration of peptides?
What is the role of Saquinavir in peptide drug design?
What is the role of Saquinavir in peptide drug design?
How does mimicking secondary structure contribute to peptidomimetic drug design?
How does mimicking secondary structure contribute to peptidomimetic drug design?
What strategy can be used to increase resistance to proteolysis while retaining intended activity of peptides?
What strategy can be used to increase resistance to proteolysis while retaining intended activity of peptides?
What is the natural target for designing inhibitors of HIV protease?
What is the natural target for designing inhibitors of HIV protease?
Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?
Why are full-sized proteins generally more resistant to enzymatic digestion than small proteins and polypeptides?
