Medical Science and Technology Innovation Center, Shandong Key Laboratory of Radiation Oncology, Shandong Cancer Hospital and Institute, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, Shandong, China.
School of Clinical and Basic Medicine, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan, Shandong, China.
Front Endocrinol (Lausanne). 2023 Sep 19;14:1220108. doi: 10.3389/fendo.2023.1220108. eCollection 2023.
The malignant lung cancer has a high morbidity rate and very poor 5-year survival rate. About 80% - 90% of protein degradation in human cells is occurred through the ubiquitination enzyme pathway. Ubiquitin ligase (E3) with high specificity plays a crucial role in the ubiquitination process of the target protein, which usually occurs at a lysine residue in a substrate protein. Different ubiquitination forms have different effects on the target proteins. Multiple short chains of ubiquitination residues modify substrate proteins, which are favorable signals for protein degradation. The dynamic balance adapted to physiological needs between ubiquitination and deubiquitination of intracellular proteins is beneficial to the health of the organism. Ubiquitination of proteins has an impact on many biological pathways, and imbalances in these pathways lead to diseases including lung cancer. Ubiquitination of tumor suppressor protein factors or deubiquitination of tumor carcinogen protein factors often lead to the progression of lung cancer. Ubiquitin proteasome system (UPS) is a treasure house for research and development of new cancer drugs for lung cancer, especially targeting proteasome and E3s. The ubiquitination and degradation of oncogene proteins with precise targeting may provide a bright prospect for drug development in lung cancer; Especially proteolytic targeted chimerism (PROTAC)-induced protein degradation technology will offer a new strategy in the discovery and development of new drugs for lung cancer.
恶性肺癌的发病率很高,5 年生存率非常低。大约 80%-90%的人类细胞中的蛋白质降解是通过泛素化酶途径发生的。具有高特异性的泛素连接酶(E3)在靶蛋白的泛素化过程中起着至关重要的作用,通常发生在底物蛋白的赖氨酸残基上。不同的泛素化形式对靶蛋白有不同的影响。多个短链的泛素化残基修饰底物蛋白,这是有利于蛋白质降解的信号。细胞内蛋白质的泛素化和去泛素化之间适应生理需求的动态平衡有利于机体的健康。蛋白质的泛素化对许多生物途径都有影响,这些途径的失衡会导致包括肺癌在内的疾病。肿瘤抑制蛋白因子的泛素化或肿瘤致癌蛋白因子的去泛素化常常导致肺癌的进展。泛素蛋白酶体系统(UPS)是肺癌新药研发的宝库,特别是针对蛋白酶体和 E3 的研究。针对癌基因蛋白的精确靶向的泛素化和降解可能为肺癌的药物开发提供广阔的前景;特别是蛋白酶体靶向嵌合体(PROTAC)诱导的蛋白质降解技术将为肺癌新药的发现和开发提供新的策略。