EGFR Inhibitor CL-387785 Suppresses the Progression of Lung Adenocarcinoma.

IF 2.4 4区生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Current molecular pharmacology Pub Date : 2023-01-01 DOI:10.2174/1874467215666220329212300

Yong Cai, Zhaoying Sheng, Zhiyi Dong, Jiying Wang

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引用次数: 1

Abstract

Objective: This study aimed to explore the influence of the irreversible EGFR inhibitor CL-387785 on invasion, metastasis, and radiation sensitization of non-small cell lung cancer cells.

Methods: The proliferation inhibitory rate at different time points was detected by MTT assay. The apoptosis of H1975 cells treated with CL-387785 was detected using flow cytometry. The invasion and migration of H1975 cells treated with CL-387785 were determined by Transwell assay and wound healing assay. The survival fraction (SF) of H1975 cells cultured with CL- 387785 under X-ray (0, 2, 4, 6, 8, and 10 Gy) was detected by cloning formation experiment, and the sensitization ratio (SER) was calculated by clicking the multi-target model to fit the cell survival curve.

Results: CL-387785 restrained H1975 cell proliferation in a concentration- and time-dependent manner. CL-387785 promoted H1975 cell apoptosis and reduced cell migration distance and the number of transmembrane cells. The SF treated by different concentrations of CL-387785 (10, 25, 50, and 100 nM) was all below 0 nM. The radiation SER of CL-387785 (10, 25, 50 and 100 nM) were 1.17, 1.39, 2.88, and 3.64, respectively.

Conclusion: The invasion and metastasis of H1975 cells were restrained by irreversible EGFR inhibitor CL-387785. CL-387785 also exhibited the effect of radiotherapy sensitization.

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EGFR抑制剂CL-387785抑制肺腺癌的进展。

目的:本研究旨在探讨不可逆EGFR抑制剂CL-387785对非小细胞肺癌细胞侵袭、转移及辐射致敏的影响。方法:采用MTT法检测不同时间点细胞增殖抑制率。流式细胞术检测CL-387785对H1975细胞凋亡的影响。采用Transwell法和创面愈合法观察CL-387785对H1975细胞的侵袭和迁移作用。通过克隆形成实验检测CL- 387785培养的H1975细胞在x射线(0、2、4、6、8、10 Gy)照射下的存活分数(SF)，点击多靶点模型拟合细胞存活曲线计算致敏比(SER)。结果:CL-387785对H1975细胞增殖具有浓度依赖性和时间依赖性。CL-387785促进H1975细胞凋亡，减少细胞迁移距离和跨膜细胞数量。不同浓度CL-387785(10、25、50、100 nM)处理后的SF均小于0 nM。CL-387785在10、25、50和100 nM的辐射SER分别为1.17、1.39、2.88和3.64。结论:不可逆EGFR抑制剂CL-387785对H1975细胞的侵袭转移有抑制作用。CL-387785也有放疗增敏作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current molecular pharmacology Pharmacology, Toxicology and Pharmaceutics-Drug Discovery

CiteScore

4.90

自引率

3.70%

发文量

112

期刊介绍： Current Molecular Pharmacology aims to publish the latest developments in cellular and molecular pharmacology with a major emphasis on the mechanism of action of novel drugs under development, innovative pharmacological technologies, cell signaling, transduction pathway analysis, genomics, proteomics, and metabonomics applications to drug action. An additional focus will be the way in which normal biological function is illuminated by knowledge of the action of drugs at the cellular and molecular level. The journal publishes full-length/mini reviews, original research articles and thematic issues on molecular pharmacology. Current Molecular Pharmacology is an essential journal for every scientist who is involved in drug design and discovery, target identification, target validation, preclinical and clinical development of drugs therapeutically useful in human disease.