Department of Medical Science, Asan Medical Institute of Convergence Science and Technology, University of Ulsan College of Medicine, Seoul 05505, Republic of Korea.
Asan Institute for Life Sciences, Asan Medical Center, Seoul 05505, Republic of Korea.
Int J Mol Sci. 2024 Jun 1;25(11):6123. doi: 10.3390/ijms25116123.
Triple-negative breast cancer (TNBC) accounts for approximately 15-20% of all breast cancer types, indicating a poor survival prognosis with a more aggressive biology of metastasis to the lung and a short response duration to available therapies. Ibulocydine (IB) is a novel (cyclin-dependent kinase) CDK7/9 inhibitor prodrug displaying potent anti-cancer effects against various cancer cell types. We performed in vitro and in vivo experiments to determine whether IB inhibits metastasis and eventually overcomes the poor drug response in TNBC. The result showed that IB inhibited the growth of TNBC cells by inducing caspase-mediated apoptosis and blocking metastasis by reducing MMP-9 expression in vitro. Concurrently, in vivo experiments using the metastasis model showed that IB inhibited metastasis of MDA-MB-231-Luc cells to the lung. Collectively, these results demonstrate that IB inhibited the growth of TNBC cells and blocked metastasis by regulating MMP-9 expression, suggesting a novel therapeutic agent for metastatic TNBC.
三阴性乳腺癌(TNBC)约占所有乳腺癌类型的 15-20%,其转移到肺部的生物学行为更具侵袭性,且对现有治疗方法的反应时间较短,因此预后较差。伊布利西布(IB)是一种新型(细胞周期蛋白依赖性激酶)CDK7/9 抑制剂前药,对各种癌细胞类型均显示出强大的抗癌作用。我们进行了体外和体内实验,以确定 IB 是否抑制转移并最终克服 TNBC 的药物反应不良。结果表明,IB 通过诱导半胱天冬酶介导的细胞凋亡和通过降低 MMP-9 表达来抑制转移,从而抑制 TNBC 细胞的生长。同时,使用转移模型的体内实验表明,IB 抑制了 MDA-MB-231-Luc 细胞向肺部的转移。总之,这些结果表明,IB 通过调节 MMP-9 表达抑制 TNBC 细胞的生长和转移,提示其可能成为转移性 TNBC 的一种新型治疗药物。