酪氨酸激酶抑制剂研究进展

来源 :华东抗肿瘤药物研究新进展与肿瘤精准治疗论坛 | 被引量 : 0次 | 上传用户:zhanggexian
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主要介绍克服酪氨酸激酶Gleevec耐药的一些进展.第一代靶点药物Gleevec耐药的主要形成机制是出现靶点点突变和基因扩增.潘景轩教授等发现了新型酪氨酸激酶抑制剂(EXEL-0862)(Blood,Leukemia,2007)、DCC-2063(PloS One,2013)、ponatinib(Mol Cancer Ther,2014;Mol Cancer,2014;Cancer Ther Biol,2014)及GZD824(JMC,2013)、S116836(Oncotarget 2014;Cancer Ther Biol,2014)能抑制突变体酪氨酸激酶的活性,并杀死耐受性白血病细胞;
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