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Antifolates are drugs which impair the function of folic acids.[1]
A well known example is Methotrexate. This is a folic acid analogue, and owing to structural similarity with it binds and inhibits the enzyme dihydrofolate reductase, and thus prevents the formation of tetrahydrofolate. Tetrahydrofolate essential for purine and pyrimidine synthesis, and this leads to inhibited production of DNA, RNA and proteins (as tetrahydrofolate is also involved in the synthesis of amino acids serine and methionine).
Other examples include trimethoprim, pyrimethamine and pemetrexed.
Since, antifolates interfere with metabolism (of nucleotides), they are categorized as antimetabolites. Their action specifically targets the fast-dividing cells, and tend to have adverse effects on the bone marrow, skin and hair.
Many new drugs are under development to reduce antifolate drug resistance.[2][3]
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References
- ^ "NCI: antifolate".
- ^ Takimoto CH (1996). "New Antifolates: Pharmacology and Clinical Applications". Oncologist 1 (1 & 2): 68–81. PMID 10387971.
- ^ Gangjee A, Jain HD, Kurup S (September 2007). "Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: part I". Anticancer Agents Med Chem 7 (5): 524–42. PMID 17896913.
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- This page was last modified on 12 July 2008, at 05:47.
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