细胞周期蛋白依赖激酶6
癌症研究
乳腺癌
三阴性乳腺癌
视网膜母细胞瘤
视网膜母细胞瘤蛋白
癌症
细胞周期
靶向治疗
免疫印迹
医学
细胞凋亡
肿瘤科
内科学
细胞周期蛋白依赖激酶
生物
生物化学
基因
作者
Jing Ji,Jingting Qin,Xiaoshuo Wang,Mingxiao Lv,Xin Hou,Aixin Jing,Jiaojiao Zhou,Lei Zuo,Wenwen Liu,Feng Jin,Qilan Qian,Yuanyuan Liu,Xiujun Wang,Yizhi Liu
出处
期刊:Anti-cancer Agents in Medicinal Chemistry
[Bentham Science]
日期:2024-01-08
卷期号:24
标识
DOI:10.2174/0118715206265751231204190204
摘要
aims: compound JHD205 is an effective breast cancer treatment and offers patients a new targeted therapy option. background: Triple-negative breast cancer (TNBC) is an aggressive, difficult-to-treat cancer subtype with a poor prognosis and an urgent need for effective targeted molecular therapies. objective: By inhibiting the phosphorylation of the retinoblastoma protein (Rb), selective CDK4/6 inhibitors can induce cell cycle G1 phase hindrance, potentially making them effective therapeutic options for TNBC. method: The compound JHD205 was synthesized based on the chemical structure of Abemaciclib, which inhibits the malignant phenotype of TNBC cells. result: Breast cancer xenograft chicken embryo models showed better tumor growth inhibition with compound JHD205 versus Abemaciclib. Meanwhile, western blot analysis showed that compound JHD205 could degrade CDK4 and CDK6 in a dose-dependent manner, while other proteins related to CDK4/6, such as p-Rb, Rb and E2F1, showed abnormal changes. Furthermore, the compound JHD205 induces apoptosis, DNA damage, and inhibits DNA repair by upregulate CASPASE 3 and p-H2AX protein levels. conclusion: As a result, compound JHD205 is a potential therapeutic strategy for the treatment of breast cancer. other: none
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