Intragenic ERBB2 kinase mutations in tumours

Intragenic ERBB2 kinase mutations in tumours
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DOI:
10.1038/431525b
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发表时间:
2004-09-30
期刊:
影响因子:
64.8
通讯作者:
Stratton, MR
Stratton, MR
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Stephens, P;Hunter, C;Stratton, MR

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蛋白激酶家族是人类癌症中最常见的突变基因家族,有缺陷的激酶正在被研究作为抗肿瘤疗法设计的有希望的目标。我们对 120 个原发性肺肿瘤中编码跨膜蛋白酪氨酸激酶 ERBB2(也称为 HER2 或 Neu)的基因进行了测序,并鉴定出 4% 在激酶结构域内有突变;在肺癌的腺癌亚型中,10%的病例有突变。迄今为止,ERBB2抑制剂已被证明对治疗肺癌无效,现在应该在肿瘤携带ERBB2突变的特定肺癌患者亚群中进行临床重新评估。
The protein-kinase family is the most frequently mutated gene family found in human cancer and faulty kinase enzymes are being investigated as promising targets for the design of antitumour therapies. We have sequenced the gene encoding the transmembrane protein tyrosine kinase ERBB2 (also known as HER2 or Neu) from 120 primary lung tumours and identified 4% that have mutations within the kinase domain; in the adenocarcinoma subtype of lung cancer, 10% of cases had mutations. ERBB2 inhibitors, which have so far proved to be ineffective in treating lung cancer, should now be clinically re-evaluated in the specific subset of patients with lung cancer whose tumours carryERBB2mutations.