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有待吸取的教训:非小细胞肺癌中激酶靶向治疗和耐药性的分子基础。

Lessons To Be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer.

机构信息

Faculty of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227, Dortmund, Germany.

出版信息

Angew Chem Int Ed Engl. 2018 Feb 23;57(9):2307-2313. doi: 10.1002/anie.201710398. Epub 2018 Jan 12.

DOI:10.1002/anie.201710398
PMID:29178586
Abstract

The treatment of non-small cell lung cancer (NSCLC) is currently experiencing a revolution. Over the last decade, the knowledge gained about the biochemical features of biomarkers and their predictive abilities has led to the development of targeted small-molecule inhibitors that present an alternative to harsh chemotherapy. The use of these new therapies has improved the quality of life and increased the survival of patients. The occurrence of inevitable drug resistance requires the constant development of precision medicine. The detailed understanding of the target biology and the search for innovative chemical approaches has encouraged investigations in this field. Herein, we review selected aspects of the molecular targets and present an overview of current topics and challenges in the rational development of small molecules to target NSCLC.

摘要

非小细胞肺癌(NSCLC)的治疗目前正在经历一场革命。在过去的十年中,人们对生物标志物的生化特征及其预测能力的了解不断深入,这导致了靶向小分子抑制剂的发展,为苛刻的化疗提供了一种替代方案。这些新疗法的应用提高了患者的生活质量并延长了其生存期。不可避免的耐药性的发生需要不断发展精准医学。对目标生物学的深入了解和对创新化学方法的探索,鼓励了该领域的研究。在此,我们综述了分子靶标的一些方面,并概述了合理开发针对 NSCLC 的小分子的当前主题和挑战。

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