Cancer Chemotherapeutic Agents Lecture 6 Dr. M Casely-Hayford: DNA Topoisomerases and Cancer Drug Development
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Questions and Answers

What is the main biological function of DNA topoisomerases?

  • Enhance DNA supercoiling
  • Synthesize new DNA strands
  • Repair damaged DNA strands
  • Cleave both strands of double-stranded DNA simultaneously (correct)

In the context of cancer drug development, what role do topoisomerases play?

  • They induce apoptosis in cancer cells
  • They repair damaged DNA in cancer cells
  • They are targets for anticancer drug development (correct)
  • They prevent cancer cell growth

How do Teniposide and etoposide relate to the mayapple plant?

  • They are used as fertilizers for the mayapple plant
  • They are toxins found in the mayapple plant
  • They are developed from the main constituent of the mayapple plant (correct)
  • They inhibit growth of the mayapple plant

What is the initial segment that Topoisomerase II binds before cleaving both DNA strands?

<p>G segment (gate segment) (D)</p> Signup and view all the answers

What happens after the ATP binds to the two N-terminal domains of Topoisomerase II?

<p>Brings the two domains together for a conformational change (C)</p> Signup and view all the answers

How does Topoisomerase II reset after hydrolysis of ATP?

<p>The G segment remains bound with the enzyme in a resealed state (B)</p> Signup and view all the answers

What is the major mechanism of antineoplastic action of podophylotoxins?

<p>Stabilizing the DNA-topo II cleavable complex (D)</p> Signup and view all the answers

Which isoform of topoisomerase II has two DNA independent binding sites?

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

What is the main difference between etoposide and teniposide?

<p>Differ in their cellular uptake due to lipophilicity (C)</p> Signup and view all the answers

What is the purpose of solubility enhancers in IV formulations of topoisomerase II inhibitors?

<p>To minimize hypersensitivity reactions (D)</p> Signup and view all the answers

When do topoisomerase II inhibitors have the most devastating effect on cells?

<p>In S or early G2 phase of the cell cycle (B)</p> Signup and view all the answers

What is the role of podophylotoxins in interacting with Topo IIα?

<p>Disrupting RNA transcription processes (B)</p> Signup and view all the answers

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