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针对肺鳞癌中的 FGFR。

Targeting FGFR in Squamous Cell Carcinoma of the Lung.

机构信息

Department of Medicine, Indiana University School of Medicine, 535 Barnhill Drive, RT 400, Indianapolis, IN, 46202, USA.

出版信息

Target Oncol. 2017 Dec;12(6):741-755. doi: 10.1007/s11523-017-0513-6.

Abstract

Unlike for adenocarcinomas of the lung, no molecular targeted therapies have yet been developed for squamous cell lung cancers, because targetable oncogenic aberrations are scarce in this tumor type. Recent discoveries have established that the fibroblast growth factor (FGF) signaling pathway plays a fundamental role in cancer development by supporting tumor angiogenesis and cancer cell proliferation via different mechanisms. Through comprehensive genomic studies, aberrations in the FGF pathway have been identified in various tumor types, including squamous cell lung cancer, making FGF receptor (FGFR) a potentially druggable target in this malignancy. Several multi-targeted tyrosine kinase inhibitors include FGFR in their target spectrum and a number of these compounds have been approved for clinical use in different cancers. Novel agents selectively targeting FGFRs have been developed and are currently under investigation in clinical trials, showing promising results. This article reviews FGFR aberrations and the clinical data involving selective and multikinase FGFR inhibitors in squamous cell lung cancer.

摘要

与肺腺癌不同,目前尚未针对鳞状细胞肺癌开发出分子靶向治疗方法,因为这种肿瘤类型中靶向致癌异常很少。最近的发现表明,成纤维细胞生长因子(FGF)信号通路通过不同的机制支持肿瘤血管生成和癌细胞增殖,在癌症发展中起着至关重要的作用。通过全面的基因组研究,已经在包括鳞状细胞肺癌在内的各种肿瘤类型中发现了 FGF 通路的异常,这使得 FGFR 成为这种恶性肿瘤中潜在的可用药靶。几种多靶点酪氨酸激酶抑制剂包括 FGFR 作为其靶点谱的一部分,其中一些化合物已被批准用于不同癌症的临床应用。新型选择性靶向 FGFR 的药物已经开发出来,并正在临床试验中进行研究,显示出有希望的结果。本文综述了 FGFR 异常以及涉及鳞状细胞肺癌中选择性和多激酶 FGFR 抑制剂的临床数据。

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