Antifolate

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Antifolates are molecules which impair the function of folic acids.[1]

A well known example is Methotrexate. This is a folic acid analogue, prevents the formation of tetrahydrofolate, essential for purine and pyrimidine synthesis, by inhibiting dihydrofolate reductase. 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 and pyrimethamine.

Many new drugs are under development to reduce antifolate drug resistance.[2][3]

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[edit] References

  1. ^ NCI: antifolate.
  2. ^ Takimoto CH (1996). "New Antifolates: Pharmacology and Clinical Applications". Oncologist 1 (1 & 2): 68–81. PMID 10387971. 
  3. ^ 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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