Department of Hepatobiliary Surgery, Central South University Xiangya School of Medicine Affiliated Haikou Hospital, Haikou, 570208, P. R. China.
Psychological Research Center, Hainan General Hospital, Haikou, 570311, P. R. China.
Cancer Gene Ther. 2021 Nov;28(10-11):1136-1149. doi: 10.1038/s41417-020-00261-w. Epub 2020 Dec 16.
Increasing evidence has suggested the crucial role cyclin-dependent kinases (CDKs) in the biology of hepatocellular carcinoma (HCC), a lethal malignancy with high morbidity and mortality. Hence, this study explored the modulatory effect of the putative cyclin-dependent kinase 11B (CDK11B)-mediated ubiquitination on HCC stem cells. The expression of CDK11B, SAM pointed domain-containing ETS transcription factor (SPDEF) and DOT1-like histone lysine methyltransferase (DOT1L) was determined by RT-qPCR and western blot analysis in HCC tissues and cells. The interaction among CDK11B, SPDEF, miR-448, and DOT1L was analyzed by Co-IP, ubiquitination-IP and ChIP assays, whereas their effects on the biological characteristics of HCC stem cells were assessed by sphere formation and colony formation assays. An in vivo xenograft tumor model was developed for validating the regulation of CDK11B in oncogenicity of HCC stem cells. We characterized the aberrant upregulation of CDK11B and downregulation SPDEF in HCC tissues and cells. CDK11B degraded SPDEF through ubiquitin-proteasome pathway, whereas SPDEF could bind to the miR-448 promoter and inhibit the expression of DOT1L by activating miR-448, whereby promoting self-renewal of HCC stem cells. Knockdown of CDK11B attenuated the self-renewal capability of HCC stem cells and their oncogenicity in vivo. These findings highlighted that blocking the CDK11B-induced degradation of SPDEF and enhancing miR-448-dependent inhibition of DOT1L may delay the progression of HCC by restraining self-renewal capability of HCC stem cells, representing novel targets for HCC management.
越来越多的证据表明,细胞周期蛋白依赖性激酶(CDKs)在肝细胞癌(HCC)的生物学中起着关键作用,HCC 是一种具有高发病率和死亡率的致命恶性肿瘤。因此,本研究探讨了假定的细胞周期蛋白依赖性激酶 11B(CDK11B)介导的泛素化对 HCC 干细胞的调节作用。通过 RT-qPCR 和 Western blot 分析检测 HCC 组织和细胞中 CDK11B、SAM 指向结构域包含 ETS 转录因子(SPDEF)和 DOT1 样组蛋白赖氨酸甲基转移酶(DOT1L)的表达。通过 Co-IP、泛素化 IP 和 ChIP 测定分析 CDK11B、SPDEF、miR-448 和 DOT1L 之间的相互作用,通过球体形成和集落形成测定评估它们对 HCC 干细胞生物学特性的影响。建立体内异种移植肿瘤模型验证 CDK11B 对 HCC 干细胞致癌性的调节作用。我们对 HCC 组织和细胞中 CDK11B 的异常上调和 SPDEF 的下调进行了特征描述。CDK11B 通过泛素蛋白酶体途径降解 SPDEF,而 SPDEF 可以结合 miR-448 启动子并通过激活 miR-448 抑制 DOT1L 的表达,从而促进 HCC 干细胞的自我更新。CDK11B 的敲低减弱了 HCC 干细胞的自我更新能力及其体内的致瘤性。这些发现强调,通过阻止 CDK11B 诱导的 SPDEF 降解和增强 miR-448 依赖性抑制 DOT1L,可能通过抑制 HCC 干细胞的自我更新能力来延缓 HCC 的进展,为 HCC 的治疗提供新的靶点。