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- FIGURE 19.2-1. The structures illustrate the variety of analogs now in
- clinical use, all based on the structure of tetrahydrofolate. The
- 2,4-diaminopteroyl glutamates (methotrexate, aminopterin, and
- 10-ethyl-10-deazaaminopterin) as well as other lipid-soluble
- 2,4-diamino structures, such as trimetrexate, inhibit dihydrofolate
- reductase. 5,10-Dideazatetrahydrofolate inhibits an entirely different
- target (GAR transformylase, an early enzyme in purine synthesis),
- whereas 5,8-dideazafolates strongly inhibit thymidylate synthase, a
- third folate-dependent enzyme. (Chabner BA, Collins JM, eds. Cancer
- chemotherapy: principles and practice. Philadelphia: JB Lippincott,
- 1990:113.)
-