2016 年第 7 期 第 14 卷

DPD酶与氟尿嘧啶类药物不良反应及疗效相关性

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关键词：DPD酶氟尿嘧啶类药物DPYD基因

• 摘要：
• 【摘要】氟尿嘧啶及其衍生物是常用的抗肿瘤药物。二氢嘧啶脱氢酶（Dihydropyrimidine dehydrogenase，DPD酶）是嘧啶代谢中的起始酶和限速酶，在氟尿嘧啶类药物的代谢中起关键作用，其活性与氟尿嘧啶类药物的毒性和疗效相关。DPD的酶活性的个体差异很大。DPD 酶部分和完全缺陷能导致严重甚至致命的药物不良反应。近年来，随着测序技术的发展，对DPD酶的研究也从酶学水平上升至基因水平。本文回顾了DPD 酶的分布、功能和检测方法，及其基因多态性与氟尿嘧啶类药物相关性。
• 5-Fluorouracil (5-Fu) and its derivants are commonly used in chemotherapy for various cancers. Dihydropyrimidine dehydrogenase (DPD) is the initial and rate-limiting enzyme in the pathway that catabolises the pyrimidines and plays an important role in the catabolism of 5-FU derivatives. DPD enzymatic activities are varied significantly from individual to individual. Partial or complete deficiency of DPD activity can lead to serious or even lethal toxicity. In recent years, with the advancement of gene sequencing techniques, the focus on the DPD has turned from enzymology to genomics. In this review, we illustrate the distribution，function，assay methods of DPD and discuss the relationship between the single-nucleotide polymorphisms of DPYD gene and 5-Fu derivatives.