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新型酪氨酸激酶抑制剂PTK787/ZK222584的研究进展 被引量：3

A novel tyrosine kinase inhibitor PTK787/ZK222584
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摘要 PTK787/ZK222584是一种新型血管内皮生长因子受体酪氨酸激酶抑制剂,通过抑制酪氨酸激酶的磷酸化,阻断信号传导,抑制肿瘤新生血管的形成从而抑制肿瘤的生长。临床前研究和临床试验研究显示该药对多种肿瘤有抗肿瘤活性,不良反应较轻。 PTK787/ZK222584 is a novel inhibitor targeting vascular endothelial growth factor （VEGF） receptor tyrosine kinases. It inhibits tumor growth with its antiangiogenic effects via blockading of VEGF signal transduction by inhibiting autophosphorylation of tyrosine kinase. Preclinical researches and clinical trails show its anti-tumor activity with slight side effects.
作者 叶泉英（综述） 陈铭珍（审校）
机构地区 广东医学院附属医院儿科研究室
出处 《国际肿瘤学杂志》 CAS 2007年第8期579-582,共4页 Journal of International Oncology
关键词 受体蛋白质酪氨酸激酶类 血管生成抑制剂 受体 血管内皮生长因子 肿瘤 Receptor protein-tyrosine kinases Angiogenesis inhibitors Receptors, vascular endothelial growth factor Neoplasms
分类号 R730.53 [医药卫生—肿瘤]
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参考文献21

  • 1Wood JM, Bold G, Buchdunger E, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res, 2000, 60(8) :2178-2189. 被引量：1
  • 2Liu Y, Poon RT, Li Q, et al. Both antiangiogenesis-and angiogenesisindependent effects are responsible for hepatocellular carcinoma growth arrest by tyrosine kinase inhibitor PTK787/ZK222584. Cancer Res, 2005, 65(9) :3691-3699. 被引量：1
  • 3Yang ZF, Poon RT, Liu Y, et al. High doses of tyrosine kinase inhibitor PTK787 enhance the efficacy of ischemic hypoxia for the treatment of hepatocellular carcinoma: dual effects on cancer cell and angiogenesis. Mol Cancer Ther, 2006,5 ( 9 ) : 2261 - 2270. 被引量：1
  • 4Yazici YD, Kim S, Jasser SA, et al. Antivascular therapy of oral tongue squamous cell carcinoma with PTK787. Laryngoscope, 2005, 115 (12) :2249-2255. 被引量：1
  • 5Solorzano CC, Baker CH, Bruns CJ, et al. Inhibition of growth and metastasis of human pancreatic cancer growing in nude mice by PTK 787/ZK222584, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinases. Cancer Biother Radiopharm, 2001, 16(5 ) : 359-370. 被引量：1
  • 6Baker CH, Solorzano CC, Fidler IJ, et al. Blockade of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling for therapy of metastatic human pancreatic cancer. Cancer Res, 2002 , 62(7) :1996-2003. 被引量：1
  • 7Drevs J, Muller-Driver R, Wittig C, et al. PTK787/ZK 222584, a specific vascular endothelial growth factor-receptor tyrosine kinase inhibitor, affects the anatomy of the tumor vascular bed and the functional vascular properties as detected by dynamic enhanced magnetic resonance imaging. Cancer Res, 2002 , 62(14) :4015-4022. 被引量：1
  • 8Schoenberger J, Grimm D, Kossmehl P, et al. Effects of PTK787/ ZK222584, a tyrosine kinase inhibitor, on the growth of a poorly differentiated thyroid carcinoma: an animal study. Endocrinology, 2004, 145(3) :1031-1038. 被引量：1
  • 9Kim S, Yazici YD, Barber SE, et al. Growth inhibition of orthotopic anaplastic thyroid carcinoma xenografts in nude mice by PTK787/ ZK222584 and CPT-11. Head Neck, 2006, 28(5) :389-99. 被引量：1
  • 10Lin B, Podar K, Gupta D, et al. The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in the bone marrow microenvironment. Cancer Res, 2002 , 62(17) :5019-5026. 被引量：1

同被引文献58

  • 1李勇,张湘茹,孙燕.多靶点抗肿瘤新药:ZD6474[J].癌症进展,2006,4(3):206-210. 被引量：19
  • 2张秀华,林莉萍,丁健.靶向血小板源生长因子受体酪氨酸激酶抑制剂的临床研究进展[J].中国新药与临床杂志,2006,25(6):454-458. 被引量：5
  • 3贡联兵.酪氨酸激酶抑制剂的进展与评价[J].中国医院用药评价与分析,2006,6(6):329-332. 被引量：9
  • 4Kabbinavar F,Hurwitz HI,Fehrenbacher L,et al.Phase Ⅱ,randomized trial comparing bevacizumab plus fluorouracil (FU)/ leucovorin (LV)with FU/ LV alone in patients with metastatic colorectal cancer[J].J Clin Oncol,2003,21 (1):60-65. 被引量：1
  • 5Wood JM,Bold G,Buchdunger E,et al.PTK787/ ZK 222584,a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases,impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration[J].Cancer Res,2000,60 (8):2178-2189. 被引量：1
  • 6Bold G,Altmann KH,Frei J,et al.New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis[J].J Med Chem,2000,43 (12):2310-2323. 被引量：1
  • 7Javaid MH,Smith GC,Martin NM,et al.4-Heteroarylmethyl substituted phthalazinone derivatives as PARP-1 inhibitors,their preparation,pharmaceutical compositions,and use in therapy:WO,2006021801[P].2006-03-02. 被引量：1
  • 8Bold G,Frei J,Traxler P,et al.Preparation of 1-arylamino-4-pyridylmethylphthalazines and analogs as VEGF receptor inhibitors:WO,9835958[P].1998-08-20. 被引量：1
  • 9ALBERT DH, TAPANG P, MAGOC TJ, et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor[J]. Mol Cancer Ther, 2006, 5(4): 995-1006. 被引量：1
  • 10WONG CI, KOH TS, SOO R, et al. Phase 1 and biomarker study of ABT-869, a multiple receptor tyrosine kinase inhibitor in patients with refractory solid malignancies[J]. J Clin Oncol, 2009, 27(28) : 4718-4726. 被引量：1

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国际肿瘤学杂志
2007年 第8期

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