期刊文献+

正在研究中的抗肿瘤新药9-硝基喜树碱 被引量:4

9-nitrocamptothecin,a new anti-tumor agent under development
下载PDF
导出
摘要 9-硝基喜树碱(9-NC)为一个半合成喜树碱衍生物,其药理作用主要表现为对拓扑异构酶Ⅰ的抑制。目前,对9-NC的研究已进入Ⅱ期或Ⅲ期临床试验,具有广泛的抗肿瘤活性,且毒性较低,是极具潜力的抗肿瘤新药。现对其药理作用、药动学、临床前研究等作一综述。 9-nitrocamptothecin(9-NC) is a semi-synthetic derivative of camptothecin, acted by inhibition of DNA topoisomerase (Topo Ⅰ). 9-NC is currently in Phase Ⅱ and Ⅲ clinical trials for variety of cancers. This paper presents the pharmacology, pharmacokinetics and pre-clinical studies of 9-NC.
出处 《中国新药杂志》 CAS CSCD 北大核心 2005年第2期226-230,共5页 Chinese Journal of New Drugs
关键词 9-硝基喜树碱 拓扑异构酶Ⅰ抑制剂 抗肿瘤药 9-nitrocamptothecin(9-NC) topoisomerase Ⅰ inhibitor anti-tumor agent
  • 相关文献

参考文献28

  • 1潘启超.抗癌新药——拓扑异构酶Ⅰ抑制剂[J].中国新药杂志,1998,7(1):6-11. 被引量:34
  • 2宋云龙,张万年,季海涛,陆信倍.DNA拓扑异构酶Ⅰ结构、功能及喜树碱类抗癌药物研究进展[J].中国药学杂志,2002,37(9):646-650. 被引量:18
  • 3Ulukan H,Swaan PW.Camptothecins:A review of theirchemotherapeutic potential[J].Drugs 2002,62(14):2039-2057
  • 4孟繁浩,巩丽颖,佟馨.抗癌药物——喜树碱类衍生物研究进展[J].生命的化学,2002,22(3):265-267. 被引量:17
  • 5Wu J, Liu LF. Processing of topoisomerase I cleavable complexes into DNA damage by transcription[J ]. Nucleic Acids Res, 1997, 25(21) :4181 - 4186.
  • 6Hinz HR, Harris NJ, Natelson EA, et al. Pharmacokinetics of the in vivo and in vitro conversion of 9-nitro-20( S)-camptothecin to 9-amino-20 ( S )-camptothecin in humans, dogs, and mice [ J ]. Cancer Res, 1994,54 (12): 3096 - 3100.
  • 7Panayotis P, Early JA, Mendoza JT, et al. Cytotoxic efficacy of 9-nitrocamptothecin in the treatment of human malignant melanoma cells in vitro [ J ]. Cancer Res, 1994, 54 ( 3 ): 771 - 776.
  • 8Hu XL, Balan KV, Ramos-DeSimone N, et al. Differential susceptibility to 9-nitrocampptothecin (9-NC)-induced apoptosis in clones derived from a human ovarian cancer cell line: possible implications in the treatment of ovarian cancer patients with 9-NC[J]. Anticancer Drugs,2003,14:427 - 436.
  • 9Chatterjee D, Schmitz I, Krueger A, et al. Induction of apoptosis in 9-nitrocamptothecin-treated DU145 human prostate carcinoma cells correlates with de novo synthesis of CD95 and CD95 ligand and down-regulation of c-FLIPshort [ J ]. Cancer Res, 2001,61 (19) :7148 - 7154.
  • 10Amorino GP,Hercules SK,Mohr PJ et al. Preclinical evaluation of the orally active camptothecin analog, RFS-2000 (9- nitro-20(S)-camptothecin) as a radiation enhancer[J]. Int J RadiationOncology Biol Phys ,2000,47(2) :503 - 509.

二级参考文献31

  • 1[1]Wang JC.DNA topoisomerases[J].Annu Rev Biochem,1996,65:635.
  • 2[2]Nitiss JL.Investigating the biological functions of DNA topoisomerases in eukaryotic cells[J].Biochim Biophys Acta,1998,1400 (1-3):63.
  • 3[3]Wallis JW,Chrebet G,Brodsky G,et al.A hyper-recombination mutation in S.cererisiae identifies a novel eukaryotic topoisomerases[J].Cell,1989,58 (2):409.
  • 4[4]Hanai R,Caron PR,Wang JC.Human TOP3:a single copy gene encoding DNA topoisomerase Ⅲ[J].Proc Natl Acad Sci USA,1996,93 (8):3653.
  • 5[5]Berger JM,Fass D,Wang JC,et al.Structural similarities between topoisomerase that cleave one or both DNA strands[J].Proc Natl Acad Sci USA,1998,95 (14):7876.
  • 6[6]Gupta M,Fujimori A,Pommier Y.Eukaryotic DNA topoisomerase Ⅰ[J].Biochim Biophys Acta,1995,1262 (1):1.
  • 7[7]Yu L,Zhu CX,Tse-Dinh YC,et al.Solution structure of the C-terminal single-stranded DNA binding domain of Escherichia coli topoisomerase I[J].Biochemistry,1995,34 (23):7622.
  • 8[8]Redinbo MR,Stewart L,Kuhn P,et al.Crystal structures of human topoisomerase Ⅰ in covalent and noncovalent complexes with DNA[J].Science,1998,279 (5356):1504.
  • 9[9]Stewart L,Redinbo MR,Qiu X,et al.A model for the mechanism of human topoisomerase Ⅰ[J].Science,1998,279 (5356):1534.
  • 10[10]Cheng C,Kussie P,Pavletich N,et al.Conservation of structure and mechanism between eukaryotic topoisomerase Ⅰ and site-specific recombinases[J].Cell,1998,92 (6):841.

共引文献66

同被引文献69

引证文献4

二级引证文献8

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部