Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway.

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL
Zhi-Yu Liu, Ruo-Tong Liu, Wen-Hao Cheng, Bo-Yu Zhang, Xing-Yu Zhang, Ying Zhou, Xiao-Qing Ye, Chun-Yun Zhou, Xiu-Jun Wang, Qian Sun, Jing Ji
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引用次数: 0

Abstract

Colorectal cancer remains a significant health threat, with its incidence continuously rising, underscoring the urgent need for the development of new therapeutic agents. In our previous research, we identified 7A, a derivative of Neratinib, as having pronounced antitumor activity. However, its specific effects and mechanisms in colorectal cancer have not been thoroughly investigated. Therefore, this study employed in vivo and in vitro experiments, utilizing techniques such as RNA sequencing, Western blotting, and PCR, to provide a comprehensive analysis of 7A's mechanism of action in colorectal cancer. The results indicate that 7A induces DNA damage and activates the P53 pathway, thereby promoting apoptosis in colorectal cancer cells. Additionally, 7A treatment significantly reduced angiogenesis and tumor weight. Our findings suggest that 7A, a Neratinib derivative, holds promise as a novel candidate for colorectal cancer therapy.

奈拉替尼衍生物 7A 通过 p53 通路诱导结肠癌细胞凋亡
结肠直肠癌仍然是一个严重的健康威胁,其发病率持续上升,因此迫切需要开发新的治疗药物。在之前的研究中,我们发现奈拉替尼的衍生物 7A 具有明显的抗肿瘤活性。然而,它在结直肠癌中的具体作用和机制尚未得到深入研究。因此,本研究采用体内和体外实验,利用 RNA 测序、Western 印迹和 PCR 等技术,全面分析了 7A 在结直肠癌中的作用机制。结果表明,7A 能诱导 DNA 损伤并激活 P53 通路,从而促进结直肠癌细胞凋亡。此外,7A 还能显著减少血管生成和肿瘤重量。我们的研究结果表明,7A(一种奈拉替尼衍生物)有望成为结直肠癌治疗的新型候选药物。
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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