12 Questions
What is the main biological function of DNA topoisomerases?
Cleave both strands of double-stranded DNA simultaneously
In the context of cancer drug development, what role do topoisomerases play?
They are targets for anticancer drug development
How do Teniposide and etoposide relate to the mayapple plant?
They are developed from the main constituent of the mayapple plant
What is the initial segment that Topoisomerase II binds before cleaving both DNA strands?
G segment (gate segment)
What happens after the ATP binds to the two N-terminal domains of Topoisomerase II?
Brings the two domains together for a conformational change
How does Topoisomerase II reset after hydrolysis of ATP?
The G segment remains bound with the enzyme in a resealed state
What is the major mechanism of antineoplastic action of podophylotoxins?
Stabilizing the DNA-topo II cleavable complex
Which isoform of topoisomerase II has two DNA independent binding sites?
Topo IIα
What is the main difference between etoposide and teniposide?
Differ in their cellular uptake due to lipophilicity
What is the purpose of solubility enhancers in IV formulations of topoisomerase II inhibitors?
To minimize hypersensitivity reactions
When do topoisomerase II inhibitors have the most devastating effect on cells?
In S or early G2 phase of the cell cycle
What is the role of podophylotoxins in interacting with Topo IIα?
Disrupting RNA transcription processes
Learn about DNA topoisomerases, their biological function, and how they are targeted for cancer drug development. Explore the mechanism of action of topoisomerase inhibitors as anticancer agents, with a focus on mayapple podophyllum peltatum.
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