Wu Wenxin, Wang Xuanyi, Ma Ruijie, Huang Shuhong, Li Hongguang, Lyu Xinxing
School of Clinical and Basic Medical Sciences, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong 250117, China.
Department of Thoracic Surgery, National Cancer Center, National Clinical Research Center for Cancer, Cancer Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100021, China.
Genes Dis. 2024 Dec 6;12(4):101483. doi: 10.1016/j.gendis.2024.101483. eCollection 2025 Jul.
Hepatocellular carcinoma (HCC) is the most prevalent type of malignant liver tumor with high morbidity and mortality and severely threatens human health and life quality. Thus, it is of great significance to investigate the molecular mechanism underlying the pathogenesis of HCC and seek biomarkers for early diagnosis. Neddylation, one of the most conserved post-translational modification types in eukaryotes, plays vital roles in the progression of HCC. During the process of neddylation, NEDD8 is covalently conjugated to its substrate proteins, thereby modulating multiple necessary biological processes. Currently, increasing evidence shows that the aberrant activation of neddylation is positively correlated with the occurrence and development of tumors and the poor clinical prognosis of HCC patients. Based on the current investigations, neddylation modification has been reported to target both the cullins and non-cullin substrates and subsequently affect HCC progression, including the virus infection, malignant transformation, tumor cell proliferation, migration and invasion ability, and tumor microenvironment. Therefore, inhibitors targeting the neddylation cascade have been developed and entered clinical trials, indicating satisfactory anti-HCC treatment effects. This review aims to summarize the latest progress in the molecular mechanism of pathologically aberrant neddylation in HCC, as well as the advances of neddylation-targeted inhibitors as potential drugs for HCC treatment.
肝细胞癌(HCC)是最常见的恶性肝肿瘤类型,发病率和死亡率高,严重威胁人类健康和生活质量。因此,研究HCC发病机制的分子机制并寻找早期诊断的生物标志物具有重要意义。Neddylation是真核生物中最保守的翻译后修饰类型之一,在HCC进展中起重要作用。在Neddylation过程中,NEDD8与其底物蛋白共价结合,从而调节多个必要的生物学过程。目前,越来越多的证据表明,Neddylation的异常激活与肿瘤的发生发展以及HCC患者的不良临床预后呈正相关。基于目前的研究,Neddylation修饰已被报道靶向cullins和非cullin底物,随后影响HCC进展,包括病毒感染、恶性转化、肿瘤细胞增殖、迁移和侵袭能力以及肿瘤微环境。因此,针对Neddylation级联反应的抑制剂已被开发并进入临床试验,显示出令人满意的抗HCC治疗效果。本综述旨在总结HCC中病理性异常Neddylation分子机制的最新进展,以及Neddylation靶向抑制剂作为HCC治疗潜在药物的研究进展。