相关实验视频

Updated: Jul 16, 2025

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib

Published on: June 26, 2019

发现YS-363是一种高度强效,选择性和口服有效的EGFR抑制剂

Pengxing He¹, Jing Jing¹, Linna Du¹

¹School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

|September 18, 2023

概括

一种新型的quinazoline化合物,YS-363,显示出对表皮生长因子受体 (EGFR) 和其突变的强烈抑制. 这种新的EGFR抑制剂在临床前模型中有效抑制了非小细胞肺癌 (NSCLC) 的生长.

科学领域:

在瘤学瘤学.
药用化学医学化学
分子生物学分子生物学

背景情况:

皮表皮生长因子受体 (EGFR) 氨酸激酶抑制剂 (TKI) 是EGFR突变非小细胞肺癌 (NSCLC) 的标准第一线治疗方法.
对当前EGFR-TKIs获得的耐药性限制了长期的临床疗效,需要新的治疗策略.
开发新的EGFR抑制剂对于克服耐药性和改善NSCLC治疗结果至关重要.

研究的目的:

为了研究一种新的基纳林化合物YS-363作为选择性可逆EGFR抑制剂的潜力.
在NSCLC模型中评估YS-363对野生类型和突变EGFR的抗癌活性.

主要方法:

在体外生化测试以确定针对野生类型和突变EGFR的IC50值.
细胞测试评估EGFR信号抑制,细胞增殖,迁移,细胞循环停止和细胞亡.
使用异种移植模型的EGFR依赖性NSCLC的体内疗效研究.

主要成果:

YS-363证明了野生型EGFR (IC50 = 0.96nM) 和L858R突变EGFR (IC50 = 0.67nM) 的强烈抑制.
该化合物表现出细胞EGFR信号的可逆抑制,抑制了癌细胞的增殖和迁移,并诱导了细胞周期停止和细胞亡.
在依赖EGFR的异种移植模型中,口服YS-363显著抑制了瘤生长.

结论:

YS-363是一种新型,选择性和可逆EGFR抑制剂,具有独特的quinazoline支架.
这种化合物对NSCLC具有显著的临床前疗效,包括对当前疗法耐药的模型.
YS-363是开发下一代针对EGFR的抗肺癌药物的有希望的候选者.

关键词:

它具有抗瘤活性.这是一种EGFR抑制剂.在 EGFR 基因酶.这里是YS-363的位置.

更多相关视频

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure

Published on: August 11, 2017

Profiling Sensitivity to Targeted Therapies in EGFR-Mutant NSCLC Patient-Derived Organoids

Profiling Sensitivity to Targeted Therapies in EGFR-Mutant NSCLC Patient-Derived Organoids

Published on: November 22, 2021

相关概念视频

Mitogens and the Cell Cycle

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...