2. Academic Validation
  3. Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway

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

  • Bioorg Med Chem Lett. 2025 Mar 1:117:130069. doi: 10.1016/j.bmcl.2024.130069.
Zhi-Yu Liu 1,  Ruo-Tong Liu 1,  Wen-Hao Cheng 1,  Bo-Yu Zhang 1,  Xing-Yu Zhang 1,  Ying Zhou 1,  Xiao-Qing Ye 1,  Chun-Yun Zhou 1,  Xiu-Jun Wang 2,  Qian Sun 3,  Jing Ji 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China.
  • 2 College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China. Electronic address: wangxiujun@jou.edu.cn.
  • 3 The First People's Hospital of Lianyungang, The First Affiliated Hospital of Kangda College of Nanjing Medical University. Lianyungang 222000, China. Electronic address: sunqian0818@126.com.
  • 4 College of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, China; College of Pharmacy and Chemistry and Chemical Engineering, Taizhou University, Taizhou, 225 300, China. Electronic address: jijing@jou.edu.cn.
PMID: 39674380 DOI: 10.1016/j.bmcl.2024.130069
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.

Keywords

Apoptosis; Colorectal cancer; Neratinib; P53.

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