Ruiz van Haperen V W, Peters G J
Department of Oncology, Free University Hospital, Amsterdam, The Netherlands.
Pharm World Sci. 1994 Apr 15;16(2):104-12. doi: 10.1007/BF01880661.
Deoxycytidine kinase is an enzyme required for the activation of, for example, cytarabine, the most widely used agent for the chemotherapy of haematological malignancies. However, deoxycytidine kinase also plays an important role in the activation of several new agents used in the treatment of leukaemia, such as cladribine. Recently, a new cytidine analogue, gemcitabine, has shown impressive activity as a single agent against several solid malignancies (ovarian cancer, non-small cell lung cancer), demonstrating that in solid tumours deoxycytidine kinase can be an important target for the activation of antimetabolites. Studies on the regulation of deoxycytidine kinase have shown that the enzyme has a complicated regulation (feedback inhibition by the product and regulation by ribonucleotides). Modulation of deoxycytidine kinase activity has already been shown to be an effective way to improve the effect of cytarabine and will probably be a target for new therapies.
脱氧胞苷激酶是一种激活某些药物（如阿糖胞苷，血液系统恶性肿瘤化疗中最常用的药物）所必需的酶。然而，脱氧胞苷激酶在几种用于治疗白血病的新型药物（如克拉屈滨）的激活过程中也起着重要作用。最近，一种新的胞苷类似物吉西他滨作为单一药物对几种实体恶性肿瘤（卵巢癌、非小细胞肺癌）显示出令人印象深刻的活性，这表明在实体肿瘤中，脱氧胞苷激酶可能是激活抗代谢物的一个重要靶点。对脱氧胞苷激酶调节的研究表明，该酶具有复杂的调节机制（产物的反馈抑制和核糖核苷酸的调节）。调节脱氧胞苷激酶活性已被证明是提高阿糖胞苷疗效的有效方法，并且可能成为新疗法的靶点。
