胸苷酸合成酶和二氢叶酸还原酶双抑制剂的研究进展

Current status of dual inhibitors of thymidylate synthase and dihydrofolate reductase

胸苷酸合成酶和二氢叶酸还原酶在肿瘤、病菌的化学治疗中都是重要靶点,已有多种抑制剂应用于临床。近年来,随着对胸苷酸合成酶和二氢叶酸还原酶作用机制和抑制剂的耐药机制的不断阐明,人们设计和合成了一系列新的抑制剂,其中胸苷酸合成酶和二氢叶酸还原酶双抑制剂成为研究的热点之一。文中对胸苷酸合成酶和二氢叶酸还原酶抑制剂药物临床应用进行综述,并介绍胸苷酸合成酶和二氢叶酸还原酶双抑制剂的研究进展。

Both thymidylate synthase and dihydrofolate reductase are important targets in antitumor or antibacterial chemotherapy. A number of their inhibitors have been applied clinically. The mechanisms of the two enzymes and the resistance mechanisms of their inhibitors have been clarified, and a series of new inhibitors have been designed and synthesized. Especially, dual inhibitors of thymidylate synthase and dlhydrofolate reductase have become a hotspot in research. This paper introduced the clinical application of thymidylate synthase and dihydrofolate reductase inhibitors, and the currently available dual inhibitors.