药效团
拉帕蒂尼
结合
表皮生长因子受体抑制剂
细胞毒性
化学
药品
癌症
癌症研究
药理学
表皮生长因子受体
医学
生物化学
乳腺癌
受体
曲妥珠单抗
体外
内科学
数学分析
数学
作者
Mengyuan Ding,Qianqian Shen,Wei Lu,Shulei Zhu
出处
期刊:Research Square - Research Square
日期:2023-04-03
标识
DOI:10.21203/rs.3.rs-2754084/v1
摘要
Abstract Throughout the reported applications of EGFR inhibitors, it is usually employed with HDAC or other targets to design multi-target inhibitors for cancer treatment. In this paper, we designed a drug conjugate that targeted EGFR&HER2 and had inhibitory activity of NAMPT simultaneously. Compound 20c significantly inhibited the EGFR&HER2 and NAMPT enzyme activities, and had comparable or even higher anti-proliferative activity than lapatinib in various cancer cells with over-expressed EGFR and HER2. Importantly, 20c was expected to overcome resistance to traditional EGFR inhibitors, so as to obtain better curative effect. This strategy is a promising method of embedding multiple pharmacophores into a single molecule, which lays a good foundation for the design and synthesis of small molecule drug conjugates with strong targeting ability and high cytotoxicity.
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