Antimetabolite

Function

Cancer treatment

Antimetabolites can be used in cancer treatment, as they interfere with DNA production and therefore cell division and the growth of tumors. Because cancer cells spend more time dividing than other cells, inhibiting cell division harms tumor cells more than other cells.

Anti-metabolites masquerade as pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the S phase (of the cell cycle), stopping normal development and division.

They also affect RNA synthesis. However, because uracil is used instead), inhibition of thymidine sythesis via thymidylate synthase selectively inhibits DNA synthesis over RNA synthesis.

Due to their efficiency, these drugs are the most widely used cytostatics.

In the ATC system, they are classified under L01B.

Antibiotics

Antimetabolites may also be para-aminobenzoic acid.^[1]

Types

Main representatives of these drugs are:

Folic acid analogues

• methionine).

Purine analogues

• 6-mercaptopurine that acts as a purine analogue and an inhibitor of DNA synthesis. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response, it affects both the cell and the humoral immunity. It also successfully suppresses autoimmunity.
• Mercaptopurine
• Thioguanine is used to treat acute leukemias and induction of remissions in acute granulocytic leukemias
• DNA ligase I and is S phase-specific (since these enzymes are highly active during DNA replication).
• cladribine are adenosine analogs which are primarily used to treat Hairy cell leukemia.

Pyrimidine analogues

• 5-fluorouracil (5FU) which inhibits thymidylate synthase.
• Floxuridine (FUDR)
• Cytosine arabinoside

See also

• Base analog

References

1. ^ "The Organic Chemistry of Drug Design and Drug Action" (2nd edition), R. B. Silverman, 2004.

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