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</p> Signup and view all the answers

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

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

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

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

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

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

    What is important in assessing ligand-based druggability?

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

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