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The Sound of Evolution
Thioguanine
Mechanism of action:
Thioguanine is a thiopurine derivative. After entering the cell, Thioguanine is converted by hypoxanthine-guanine phosphoribosyltransferase into active metabolites known as thioguanine nucleotides. These thioguanine nucleotides inhibit several key enzymes in the purine synthesis pathway, reducing the production of GMP and AMP and depriving rapidly dividing tumor cells of sufficient nucleotides.
Reference(s):
1. Schwartz EL et al. (1983). Induction of leukemia cell differentiation by chemotherapeutic agents. Adv Enzyme Regul.
2. Riscoe MK et al. (1989). Purine metabolism as a target for leukemia chemotherapy. Blood Rev.
3. Sahasranaman S et al. (2008). Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol.
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