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Thioguanine

硫鳥嘌呤

Mechanism of action:

Thioguanine 是一種硫嘌呤(thiopurine)衍生物。Thioguanine 進入細胞後,由次黃嘌呤-鳥嘌呤磷酸核苷轉移酶(hypoxanthine-guanine phosphoribosyltransferase)轉化為活性代謝物 thioguanine nucleotides。Thioguanine nucleotides 會抑制多個嘌呤合成途徑中的重要酵素,導致 GMP、AMP 生成下降,使快速分裂的腫瘤細胞無法獲得足夠核苷酸。

​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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