Cytidine Nucleosides and Their Analogs

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Questions and Answers

What primary mechanism enables the compounds described to exert their effect?

  • Disrupting the cell membrane, leading to cell lysis
  • Integrating themselves into DNA (correct)
  • Directly binding to and deactivating mRNA
  • Inhibiting protein synthesis by binding to ribosomes

What enzymatic activity is directly targeted by these compounds?

  • Telomerases
  • Histone deacetylases (HDACs)
  • DNA methyltransferases (DNMTs) (correct)
  • Topoisomerases

What structural characteristic do the describe compounds share with cytidine?

  • They contain a ribose sugar.
  • They possess a unique phosphate group modification.
  • They are lipid-based molecules.
  • They are chemical analogues of the nucleoside. (correct)

What factor historically limited the widespread use of these compounds, particularly in solid tumors?

<p>The significant toxicities associated with high drug doses (A)</p> Signup and view all the answers

What approach has led to a resurgence in the clinical interest and application of these compounds?

<p>Employing low-dose regimens (A)</p> Signup and view all the answers

Flashcards

Cytidine Analogues

Chemical compounds similar to cytidine that integrate into DNA.

Antimetabolites

Substances that interfere with DNA synthesis by mimicking nucleotides.

DNA Methyltransferases (DNMTs)

Enzymes that add methyl groups to DNA, affecting gene expression.

Toxicity in Cancer Treatment

Adverse effects caused by high doses of drugs in cancer therapies.

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Low Dose Regimens

Treatment strategies using smaller amounts of drugs to minimize side effects.

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Study Notes

Analogues of Cytidine Nucleoside

  • These compounds are chemically similar to cytidine nucleosides.
  • They need to be incorporated into DNA to function.

Discovery and Initial Use

  • Developed as anti-metabolites in the 1960s.
  • Found to inhibit DNA methyltransferases (DNMTs), targeting DNA.

Toxicity and Clinical Use

  • High doses cause significant toxicity in cancer patients.
  • Limited use, particularly for solid tumors, due to toxicity.
  • Recent clinical trials show promise with low-dose regimens.
  • Low doses result in improved clinical outcomes with reduced side effects.

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