Cancer Chemotherapy - Anti-metabolites Flashcards
What are Antimetabolites?
Toxic analogues of essential precursors for macromolecules
Antimetabolites are designed for what 2 purposes?
- To inhibit essential enzymes
- Distrupt the formation of macromolecules (includes DNA and RNA)
Folic acid if important in the formation of _________ _________
Pyrimidine bases
Pyrimidine bases are involved in the synthesis of _____ , ______ and ________.
DNA / RNA / Proteins
5-FdUMP (5-fluoro-deoxyuridine monophosphate) is MORE POTENT than 5-FU (5-fuorouracil). True or False
True - Therefor 5-FU needs to be metabolised to 5-FdUMP.
5-FU is incorporated into ______ and ______.
RNA and DNA
Why is 5-FU less incorporated into DNA?
5-FU is a uracil analogue
Capecitabine is a prodrug of _________
5-FU
Antifolates inhibit the synthesis or DNA, RNA and what else?
Thymidylates and proteins
What do Anti-metabolites inhibit?
They inhibit metabolic processes that generate nucleic acids required in proliferating cells
5-FU generates a ‘frozen’ transition state complex when inhibiting….
Thymidylate synthase
What are newer versions of anti-metabolites called?
Prodrugs