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CUDC-101 是一种针对 EGFR 过表达膀胱癌细胞的潜在靶向抑制剂。

CUDC‑101 is a potential target inhibitor for the EGFR‑overexpression bladder cancer cells.

机构信息

Translational Medicine Center, Huaihe Hospital of Henan University, Henan University, Kaifeng, Henan 475000, P.R. China.

School of Pharmacy, The First Affiliated Hospital of Henan University, Henan University, Kaifeng, Henan 475000, P.R. China.

出版信息

Int J Oncol. 2023 Dec;63(6). doi: 10.3892/ijo.2023.5579. Epub 2023 Oct 13.

Abstract

Bladder cancer is one of the most common urological malignancies worldwide. The molecular mechanism underlying its development is complex, but its carcinogenesis has been proposed to occur with cell proliferation and resistance to apoptosis, driven by the signaling activity of abundant EGFR and receptor tyrosine‑protein kinase erbB‑2. In the present study, T24 bladder cancer cell lines with EGFR‑overexpression were constructed, before the multi‑target inhibitor CUDC‑101 was used to investigate its potential as a targeted therapeutic agent for bladder cancer using chemosensitivity methods. The results showed that CUDC‑101 induced cytotoxic effects, inhibited growth vitality and proliferation in a dose‑dependent manner. CUDC‑101 also altered the skeletal morphology and microfilament structure, while blocking cell cycle progression and causing apoptosis. These results supported the proposed cytotoxic effects of CUDC‑101, in addition to its inhibitory effects on cell division and proliferation in EGFR‑overexpressing bladder cancer cells. Therefore CUDC‑101 may to be a potential therapeutic option for the treatment of bladder cancer.

摘要

膀胱癌是全世界最常见的泌尿系统恶性肿瘤之一。其发展的分子机制复杂,但据推测其发生是由于大量表皮生长因子受体(EGFR)和表皮生长因子受体酪氨酸蛋白激酶 erbB-2 的信号活性驱动细胞增殖和抗细胞凋亡。在本研究中,构建了 EGFR 过表达的 T24 膀胱癌细胞系,然后采用多靶点抑制剂 CUDC-101 进行研究,通过化疗敏感性方法来评估其作为膀胱癌靶向治疗药物的潜力。结果表明,CUDC-101 呈剂量依赖性诱导细胞毒性作用,抑制生长活力和增殖。CUDC-101 还改变了细胞骨架形态和微丝结构,同时阻断细胞周期进程并诱导细胞凋亡。这些结果支持 CUDC-101 的拟议细胞毒性作用,除了对 EGFR 过表达膀胱癌细胞的细胞分裂和增殖的抑制作用。因此,CUDC-101 可能是治疗膀胱癌的一种潜在治疗选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ebda/10622178/f981002abff8/ijo-63-06-05579-g00.jpg

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