Understanding Druggability in Drug Discovery

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Questions and Answers

What is the main focus of methods for assessing druggability mentioned in the text?

  • Identifying drug-like ligands
  • Assessing the likelihood of proteins binding drug-like molecules (correct)
  • Prioritizing proteins in the human genome
  • Predicting protein crystal structures

Which algorithm is specifically mentioned as being trained on a set of binding sites from the Protein Data Bank?

  • DogSiteScorer
  • Homology-based method
  • DailyMed.gov
  • PocketFinder (correct)

What does the text suggest as an issue with ligand/structure-based druggability assessment methods?

  • They provide the highest degree of confidence
  • They are useful for all novel targets
  • They rely on protein sequences
  • They are not applicable when crystal structures are unavailable (correct)

Which database is NOT mentioned as a source for high affinity drug-like compounds in the text?

<p>TTD (C)</p> Signup and view all the answers

What is a key property used in structure-based prediction methods to assess druggability?

<p>Surface area (B)</p> Signup and view all the answers

Why are methods needed to prioritize proteins in the human genome according to the text?

<p>To assess proteins that may be 'druggable' without crystal structures (C)</p> Signup and view all the answers

What are the key properties a protein's binding site should have to bind drug-like compounds?

<p>Appropriate size, buried, not too polar, large exposed polar sites (C)</p> Signup and view all the answers

Why is it important to assess druggability when identifying potential drug targets?

<p>To avoid failure in later stages due to poor pharmacokinetic properties of compounds (C)</p> Signup and view all the answers

How can protein druggability be assessed based on structural analysis?

<p>By checking the protein Data Bank for predictions (B)</p> Signup and view all the answers

What is one reason choosing a target that doesn't bind small molecules can lead to failure?

<p>Potential failure in identifying clinical candidates (C)</p> Signup and view all the answers

What percentage of human genome is estimated to be druggable with a small molecule approach?

<p>~15% (A)</p> Signup and view all the answers

In assessing druggability, what type of studies are used to relate genes/proteins to disease?

<p>A combination of sequencing/GWAS studies, expression studies, and proteomics/metabolomics studies (C)</p> Signup and view all the answers

What is another term sometimes used instead of 'druggability'?

<p>Ligandability (B)</p> Signup and view all the answers

Which of the following is NOT one of Lipinski's Rule of Five for drug-likeness?

<p>LogP &lt; 3 (D)</p> Signup and view all the answers

What do the Lipinski's Rule of Five suggest may lead to poor absorption and permeability?

<p>High number of H-bond Acceptors (A)</p> Signup and view all the answers

Which term describes the likelihood of finding orally bioavailable small molecules that bind to a particular target in a disease-modifying way?

<p>Druggability (D)</p> Signup and view all the answers

What is important in assessing ligand-based druggability?

<p>Hydrophobicity (A)</p> Signup and view all the answers

Which parameter is crucial in determining the ability of a protein target to bind small molecules with high affinity?

<p>H-bond interactions between the ligand and protein (A)</p> Signup and view all the answers

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