Song Ying-Qi, Wu Chun, Wu Ke-Jia, Han Quan-Bin, Miao Xiang-Min, Ma Dik-Lung, Leung Chung-Hang
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau.
Department of Chemistry, Hong Kong Baptist University, Kowloon, Hong Kong.
Front Cell Dev Biol. 2021 May 12;9:665646. doi: 10.3389/fcell.2021.665646. eCollection 2021.
The ubiquitin-proteasome system oversees cellular protein degradation in order to regulate various critical processes, such as cell cycle control and DNA repair. Ubiquitination can serve as a marker for mutation, chemical damage, transcriptional or translational errors, and heat-induced denaturation. However, aberrant ubiquitination and degradation of tumor suppressor proteins may result in the growth and metastasis of cancer. Hence, targeting the ubiquitination cascade reaction has become a potential strategy for treating malignant diseases. Meanwhile, computer-aided methods have become widely accepted as fast and efficient techniques for early stage drug discovery. This review summarizes ubiquitination regulators that have been discovered via virtual screening and their applications for cancer treatment.
泛素-蛋白酶体系统负责监督细胞内蛋白质的降解，以调控各种关键过程，如细胞周期控制和DNA修复。泛素化可作为突变、化学损伤、转录或翻译错误以及热诱导变性的标志物。然而，肿瘤抑制蛋白的异常泛素化和降解可能导致癌症的生长和转移。因此，靶向泛素化级联反应已成为治疗恶性疾病的一种潜在策略。同时，计算机辅助方法作为早期药物发现的快速有效技术已被广泛接受。本文综述了通过虚拟筛选发现的泛素化调节剂及其在癌症治疗中的应用。
