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

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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?

G segment (gate segment) (D) Signup and view all the answers

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

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

How does Topoisomerase II reset after hydrolysis of ATP?

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

What is the major mechanism of antineoplastic action of podophylotoxins?

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

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

Topo IIα (B) Signup and view all the answers

What is the main difference between etoposide and teniposide?

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

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

To minimize hypersensitivity reactions (D) Signup and view all the answers

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

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

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

Disrupting RNA transcription processes (B) Signup and view all the answers