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首个酪氨酸激酶抑制剂药物Gleevec 被引量：6

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摘要 GleevecTM(原名STI5 71)是第一个被美国食品与药物管理局 (FDA)批准上市的酪氨酸激酶抑制剂 ,能选择性地抑制慢性髓样白血病 (CML)患者的Bcr Abl蛋白酪氨酸激酶活性 ,对治疗CML取得了很好的疗效。Gleevec治疗CML的实验研究和临床试验都显示出令人满意的结果 ,分子作用和耐药机制的研究也有了新的认识和发现。该药物的开发成功 ,带动了酪氨酸激酶抑制剂的研究热潮 。
作者 郭晓宁 丁健
机构地区 中国科学院上海生命科学院上海药物研究所肿瘤药理实验室
出处 《生理科学进展》 CAS CSCD 北大核心 2003年第2期183-186,共4页 Progress in Physiological Sciences
关键词 酪氨酸激酶抑制剂 G1eevec 抗肿瘤药 慢性髓样白血病
分类号 R979.1 [医药卫生—药品] R73 [医药卫生—肿瘤]
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参考文献9

  • 1Buchdunger E, Matter A, Druker BJ. Bcr-Abl inhibition as a modality of CML therapeutics. Biochim Biophys Acta,2001, 1551 : M11-8.
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同被引文献116

  • 1主鸿鹄,徐开林.慢性髓性白血病研究现状[J].白血病．淋巴瘤,2006,15(4):303-306. 被引量：3
  • 2郑斌,危晴岚,刘茂柏.甲磺酸伊马替尼临床研究概况[J].海峡药学,2006,18(6):78-80. 被引量：12
  • 3Julia M Brain,Anuraag Saksena,Pierre Laneuville.The kinase inhibitor STI571 reverses the Bcr-Abl induced point mutation frequencies observed in pre-leukemic P190 Bcr-Abl transgenic mice[J].Leukemia Research,2002,26:1 011-1 016.
  • 4Isabelle Gaston,Paula E Stenberg,Arun Bhat,et al.Abl kinase but not PI3-kinase links to the cytoskeletal defects in Bcr-Abl transformed cells[J].Experimental Hematology,2000,28:77-86.
  • 5Michael E O'Dwayer,Brian J Druker.STI571:an inhibitor of the BCR-ABL tyrosine kinase for the treatment of chronic myelogenous leukaemia[J].Lancet Oncol,2000,(1):207-211.
  • 6Anjali S Advani,Ann Marie Pendergast.Bcr-Abl variants:biological and clinical aspects[J].Leukemia Research,2002,(26):713-720.
  • 7Druker B J,Talpaz M,Rasta D J,et al.Efficacy and safety of a specific inhibitor of the Bcr-Abl tyrosine kinase in chronic myeloid leukemia[J].The New England Journal of Medicine,2001,344:1 031-1 037.
  • 8Talpaz M,Silver R T,Durker B J,et al.Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia:results of a phase 2 study[J].Blood 2002,99:1 928-1 937.
  • 9Dorothea Gadzicki,Nils von Neuhoff,Doris Steinemann,et al.Bcr-Abl gene amplification and overexpression in a patient with chronic myeloid leukemia treated with imatinib[J].Cancer Genetics and Cytogenetics,2005,159:164-167.
  • 10Daniella Yeheskely-Hayon,Ronit Regev,Gera D Eytan,et al.The tyrosine kinase inhibitors imatinib and AG957 reverse multidrug resistance in a chronic myelogenous leukemia cell line[J].Leukemia Research,2005,29:793-802.

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生理科学进展
2003年 第2期

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