Research on antitumor effects of small molecule inhibitors of deubiquitinases: new progress and new ideas
10.16438/j.0513-4870.2021-1118
- VernacularTitle:去泛素化酶小分子抑制剂抗肿瘤作用研究: 新进展和新思路
- Author:
Xiang-ning LIU
;
Jia-min DU
;
Mei-jia QIAN
;
Xiao-wu DONG
;
Bo YANG
;
Hong ZHU
;
Qiao-jun HE
- Publication Type:Research Article
- Keywords:
ubiquitin proteasome pathway;
eubiquitinase;
eubiquitinase inhibitor;
new anti-tumor target;
allosteric regulation
- From:
Acta Pharmaceutica Sinica
2022;57(3):547-556
- CountryChina
- Language:Chinese
-
Abstract:
The abnormality of ubiquitin proteasome pathway is an important factor leading to the imbalance of protein homeostasis. In this process, the deubiquitinase responsible for removing the ubiquitin chain of protein substrate is very important. Its abnormal activity or expression can cause the functional changes of key oncogenic/tumor suppressor proteins, which directly or indirectly lead to the occurrence, development and malignant evolution of tumors. Based on this, the discovery and research of small molecule inhibitors targeting deubiquitinases have become a hot field of anti-tumor candidate drugs. This review will focus on the regulatory effect and mechanism of ubiquitin proteasome pathway, especially deubiquitinase on tumor, introduce the application of deubiquitinase small molecule inhibitors in tumor treatment, and discuss the research status and latest progress of small molecule inhibitors, so as to provide ideas for the research of new anti-tumor strategies based on deubiquitinase.
