Pharmacological Control of RTK Activation in Tumors
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Questions and Answers

Which protein is the first element in the MAPK cascade and the first oncogenic protein discovered in human tumors?

  • KRAS
  • Ras (correct)
  • HRAS
  • Raf
  • What is the common mutation found in K-Ras that leads to its activation?

  • Deletion of a codon
  • Insertion of an extra codon
  • Silent mutation in the codon for alanine
  • SNP in the codon for glycine in position 12 (correct)
  • Which Ras isoform was identified in human neuroblastoma?

  • TRAS
  • KRAS
  • NRAS (correct)
  • HRAS
  • What effect does the SNP in K-Ras have on the protein?

    <p>It becomes insensitive to the activity of GAP helper protein</p> Signup and view all the answers

    Which type of tumors are highly associated with activating mutations in RAS?

    <p>Pancreatic and lung cancer</p> Signup and view all the answers

    What was the initial approach to inhibiting Ras?

    <p>Inhibiting Ras by preventing its membrane association</p> Signup and view all the answers

    Why were statins tested in relation to Ras inhibition?

    <p>They inhibit the HMG-CoA reductase, involved in the synthesis of prenyl substrates</p> Signup and view all the answers

    Why did GTP analogues fail to show expected efficacy as inhibitors of Ras?

    <p>They didn't act as competitive inhibitors of GTP required for RAS activation</p> Signup and view all the answers

    What was the main reason for considering Ras an undruggable target for a long time?

    <p>The protein has a relative smooth/flat surface, lacking a well-defined binding pocket</p> Signup and view all the answers

    Why did inhibitors targeting enzymes involved in post-translational lipid modification fail?

    <p>The enzymes were not specific to Ras prenylation process</p> Signup and view all the answers

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