中国肺癌杂志Issue(9):592-598,7.DOI:10.3779/j.issn.1009-3419.2015.09.11
EGFR-L861Q突变对TKI类药物敏感性预测分析及病例报道
Analyzing the Sensitivity of EGFR-L861Q Mutation to TKIs and A Case Report
摘要
Abstract
Background and objective hTe signiifcant effcacy of tyrosine kinase inhibitors (TKIs) has been ap-proved for advanced non-small cell lung cancer (NSCLC) patients with activating epidermal growth factor receptor (EGFR) mutations. No clear evidence exists that EGFR-L861Q is sensitive to TKIs, and the best treatment for NSCLC patients with EGFR-L861Q mutation is undetermined. hTis study aims to discuss the best treatment for advanced NSCLC patients with EG-FR-L861Q mutation by analyzing the differences among the structures of wild-type EGFR, activating mutant EGFR-L858R, and EGFR-L861Q mutation. Method The protein structures of wild-type EGFR were reconstructed. EGFR-L858R and EGFR-L861Q mutation were activated. hTe differences among the three kinds of protein conformation were analyzed using homologous modeling technique. Results hTe structure of EGFR-L858R and wild-type EGFR exhibited notable distinctions. hTe structure of EGFR-L861Q mutation was different compared with wild-type EGFR and activating mutant EGFR-L858R protein conformations. NSCLC patients with EGFR-L861Q mutation were given chemotherapy as the ifrst-line of therapy, and TKIs were applied to maintain treatment when the tumor is unchanged. Effect evaluation result was improved when the lung computed tomography lesions were reviewed. Conclusion hTe analysis of the protein conformation of EGFR-L861Q muta-tion and the curative effect of chemotherapy with TKIs could help predict the sensitivity of EGFR-L861Q to TKIs. Combining the analysis with a clinical case, maintenance treatment with TKIs may achieve satisfactory curative effect in advanced NSCLC patients who have achieved disease control atfer ifrst-line chemotherapy.关键词
肺肿瘤/EGFR-L861Q突变/空间构象/酪氨酸激酶抑制剂Key words
Lung neoplasms/EGFR-L861Q mutation/Protein conformation/Tyrosine kinase inhibitors引用本文复制引用
王星星,董雨桐,梁婷婷,张雄基,马克威,崔永生..EGFR-L861Q突变对TKI类药物敏感性预测分析及病例报道[J].中国肺癌杂志,2015,(9):592-598,7.基金项目
本研究受国家自然科学基金项目(No.81372870)资助 ()