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酪氨酸-DNA磷酸二酯酶抑制剂的研究进展

黄亚辉 董国强 张万年 盛春泉

黄亚辉, 董国强, 张万年, 盛春泉. 酪氨酸-DNA磷酸二酯酶抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
引用本文: 黄亚辉, 董国强, 张万年, 盛春泉. 酪氨酸-DNA磷酸二酯酶抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
HUANG Yahui, DONG Guoqiang, ZHANG Wannian, SHENG Chunquan. Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
Citation: HUANG Yahui, DONG Guoqiang, ZHANG Wannian, SHENG Chunquan. Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003

酪氨酸-DNA磷酸二酯酶抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.003
基金项目: 国家优秀青年科学基金(No.81222044)

Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors

  • 摘要: 酪氨酸-DNA磷酸二酯酶Ⅰ(tyrosyl-DNA-phosphodiesterase Ⅰ,TdpⅠ)是一个具有催化3'磷酸酪氨酸键水解活性的蛋白质,该键在拓扑异构酶Ⅰ(topoisomerase Ⅰ, TopⅠ)与DNA相互作用时就会形成。由于TdpⅠ具有修复TopⅠ-DNA复合物、抵消TopⅠ抑制剂作用的功能,因而与TopⅠ共同被认作是潜在治疗靶标。TdpⅠ抑制剂不仅与TopⅠ抑制剂(喜树碱类)起到协同作用,还能增强博来霉素、TopⅡ抑制剂(依托泊苷、多柔比星)以及DNA烷化剂作用。综述目前报道的TdpⅠ抑制剂研究进展,重点介绍其作用机制、生物活性及构效关系。
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酪氨酸-DNA磷酸二酯酶抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.003
    基金项目:  国家优秀青年科学基金(No.81222044)

摘要: 酪氨酸-DNA磷酸二酯酶Ⅰ(tyrosyl-DNA-phosphodiesterase Ⅰ,TdpⅠ)是一个具有催化3'磷酸酪氨酸键水解活性的蛋白质,该键在拓扑异构酶Ⅰ(topoisomerase Ⅰ, TopⅠ)与DNA相互作用时就会形成。由于TdpⅠ具有修复TopⅠ-DNA复合物、抵消TopⅠ抑制剂作用的功能,因而与TopⅠ共同被认作是潜在治疗靶标。TdpⅠ抑制剂不仅与TopⅠ抑制剂(喜树碱类)起到协同作用,还能增强博来霉素、TopⅡ抑制剂(依托泊苷、多柔比星)以及DNA烷化剂作用。综述目前报道的TdpⅠ抑制剂研究进展,重点介绍其作用机制、生物活性及构效关系。

English Abstract

黄亚辉, 董国强, 张万年, 盛春泉. 酪氨酸-DNA磷酸二酯酶抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
引用本文: 黄亚辉, 董国强, 张万年, 盛春泉. 酪氨酸-DNA磷酸二酯酶抑制剂的研究进展[J]. 药学实践与服务, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
HUANG Yahui, DONG Guoqiang, ZHANG Wannian, SHENG Chunquan. Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
Citation: HUANG Yahui, DONG Guoqiang, ZHANG Wannian, SHENG Chunquan. Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 298-302. doi: 10.3969/j.issn.1006-0111.2015.04.003
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