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硫嘌呤

硫代鸟嘌呤
巯嘌呤
硫唑嘌呤

硫嘌呤(thiopurine)是嘌呤抗代谢物,常用来治疗急性淋巴性白血病自体免疫性疾病(如克隆氏症类风湿性关节炎),其在体内需经代谢转化成具有生物活性的巯基鸟嘌呤核苷酸,发挥杀死肿瘤细胞的作用,也常用在接受器官移植的患者。一旦硫嘌呤类药物在体内代谢通路中的关键酶存在单核苷酸多态性或发生功能突变,肿瘤细胞就会耐受硫嘌呤类药物而产生耐药复发。

非金属依赖性的硫嘌呤甲基转移酶会催化硫嘌呤[1],使其甲基化,在硫原子上增加一个甲基,过程中提供甲基的是S-腺苷甲硫氨酸,后者同时被转化成S-腺苷-L-高半胱氨酸

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参考资料

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  1. ^ Sahasranaman S, Howard D, Roy S. Clinical pharmacology and pharmacogenetics of thiopurines. Eur. J. Clin. Pharmacol. August 2008, 64 (8): 753–67. PMID 18506437. doi:10.1007/s00228-008-0478-6. 

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硫嘌呤
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