Podcast
Questions and Answers
What primary mechanism enables the compounds described to exert their effect?
What primary mechanism enables the compounds described to exert their effect?
What enzymatic activity is directly targeted by these compounds?
What enzymatic activity is directly targeted by these compounds?
What structural characteristic do the describe compounds share with cytidine?
What structural characteristic do the describe compounds share with cytidine?
What factor historically limited the widespread use of these compounds, particularly in solid tumors?
What factor historically limited the widespread use of these compounds, particularly in solid tumors?
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What approach has led to a resurgence in the clinical interest and application of these compounds?
What approach has led to a resurgence in the clinical interest and application of these compounds?
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Flashcards
Cytidine Analogues
Cytidine Analogues
Chemical compounds similar to cytidine that integrate into DNA.
Antimetabolites
Antimetabolites
Substances that interfere with DNA synthesis by mimicking nucleotides.
DNA Methyltransferases (DNMTs)
DNA Methyltransferases (DNMTs)
Enzymes that add methyl groups to DNA, affecting gene expression.
Toxicity in Cancer Treatment
Toxicity in Cancer Treatment
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Low Dose Regimens
Low Dose Regimens
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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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Description
Explore the properties and clinical implications of cytidine nucleosides and their analogues. Learn about their discovery as anti-metabolites, their mechanism of action in inhibiting DNMTs, and recent advancements in low-dose clinical trials that improve patient outcomes.
