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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。
  • [1] Wang JC. DNA topoisomerases[J]. Annu Rev Biochem, 1996, 65:635-692.
    [2] Pommier Y. Topoisomerase I inhibitors: camptothecins and beyond[J]. Nat Rev Cancer, 2006, 6(10):789-802.
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    [7] Pouliot JJ, Yao KC, Robertson CA, et al. Yeast gene for a Tyr-DNA phosphodiesterase that repairs topoisomerase I complexes[J]. Science, 1999, 286(5439):552-555.
    [8] El-Khamisy SF, Saifi GM, Weinfeld M, et al. Defective DNA single-strand break repair in spinocerebellar ataxia with axonal neuropathy-1[J]. Nature, 2005, 434(7029):108-113.
    [9] Plo I, Liao ZY, Barcelo JM, et al. Association of XRCC1 and tyrosyl DNA phosphodiesterase (Tdp1) for the repair of topoisomerase I-mediated DNA lesions[J]. DNA Repair (Amst), 2003, 2(10):1087-1100.
    [10] Whitehouse CJ, Taylor RM, Thistlethwaite A, et al. XRCC1 stimulates human polynucleotide kinase activity at damaged DNA termini and accelerates DNA single-strand break repair[J]. Cell, 2001, 104(1):107-117.
    [11] Pommier Y, Redon C, Rao VA, et al. Repair of and checkpoint response to topoisomerase I-mediated DNA damage[J]. Mutat Res, 2003, 532(1-2):173-203.
    [12] Takashima H, Boerkoel CF, John J, et al. Mutation of TDP1, encoding a topoisomerase I-dependent DNA damage repair enzyme, in spinocerebellar ataxia with axonal neuropathy[J]. Nat Genet, 2002, 32(2):267-272.
    [13] El-Khamisy SF, Katyal S, Patel P, et al. Synergistic decrease of DNA single-strand break repair rates in mouse neural cells lacking both Tdp1 and aprataxin[J]. DNA Repair (Amst), 2009, 8(6):760-766.
    [14] Das BB, Antony S, Gupta S, et al. Optimal function of the DNA repair enzyme TDP1 requires its phosphorylation by ATM and/or DNA-PK[J]. EMBO J, 2009, 28(23):3667-3680.
    [15] Katyal S, el-Khamisy SF, Russell HR, et al. TDP1 facilitates chromosomal single-strand break repair in neurons and is neuroprotective in vivo[J]. EMBO J, 2007, 26(22):4720-4731.
    [16] Hirano R, Interthal H, Huang C, et al. Spinocerebellar ataxia with axonal neuropathy: consequence of a Tdp1 recessive neomorphic mutation?[J]. EMBO J, 2007, 26(22):4732-4743.
    [17] Barthelmes HU, Habermeyer M, Christensen MO, et al. TDP1 overexpression in human cells counteracts DNA damage mediated by topoisomerases I and II[J]. J Biol Chem, 2004, 279(53):55618-55625.
    [18] Nivens MC, Felder T, Galloway AH, et al. Engineered resistance to camptothecin and antifolates by retroviral coexpression of tyrosyl DNA phosphodiesterase-I and thymidylate synthase[J]. Cancer Chemother Pharmacol, 2004, 53(2):107-115.
    [19] Pommier Y, Barcelo JM, Rao VA, et al. Repair of topoisomerase I-mediated DNA damage[J]. Prog Nucleic Acid Res Mol Biol, 2006, 81:179-229.
    [20] Dexheimer TS, Antony S, Marchand C, et al. Tyrosyl-DNA phosphodiesterase as a target for anticancer therapy[J]. Anticancer Agents Med Chem, 2008, 8(4):381-389.
    [21] Liao Z, Thibaut L, Jobson A, et al. Inhibition of human tyrosyl-DNA phosphodiesterase by aminoglycoside antibiotics and ribosome inhibitors[J]. Mol Pharmacol, 2006, 70(1):366-372.
    [22] Antony S, Marchand C, Stephen AG, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1[J]. Nucleic Acids Res, 2007, 35(13):4474-4484.
    [23] Marchand C, Lea WA, Jadhav A, et al. Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay[J]. Mol Cancer Ther, 2009, 8(1):240-248.
    [24] Dexheimer TS, Gediya LK, Stephen AG, et al. 4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesulfonate) (NSC 88915) and related novel steroid derivatives as tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors[J]. J Med Chem, 2009, 52(22):7122-7131.
    [25] Weidlich IE, Dexheimer T, Marchand C, et al. Inhibitors of human tyrosyl-DNA phospodiesterase (hTdp1) developed by virtual screening using ligand-based pharmacophores[J]. Bioorg Med Chem, 2010, 18(1):182-189.
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    [27] Nguyen TX, Morrell A, Conda-Sheridan M, et al. Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors[J]. J Med Chem, 2012, 55(9):4457-4478.
    [28] Sirivolu VR, Vernekar SK, Marchand C, et al. 5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl-DNA phosphodiesterase I[J]. J Med Chem, 2012, 55(20):8671-8684.
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  • 收稿日期:  2014-07-14
  • 修回日期:  2014-10-27

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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