Progress of drugs targeting E3 ubiquitin ligase
10.3969/j.issn.1001-1978.2021.06.003
- Author:
Nian-Ying SHANG
1
;
Ying PENG
1
;
Chun-Yang ZHAO
2
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College
2. Center for Drug Evaluation, National Medical Product Administration
- Publication Type:Journal Article
- Keywords:
Alzheimer' s disease;
E3 ubiquitin ligase;
enzyme activators;
enzyme inhibitors;
inflammatory bowel diseases;
Parkinson's disease;
proteolysis-targeting chimera
- From:
Chinese Pharmacological Bulletin
2021;37(6):749-755
- CountryChina
- Language:Chinese
-
Abstract:
The ubiquitin-proteasome pathway is one of the most important pathways of cell protein degradation in eukaryotes, and plays an important role in the regulation of cell proliferation, differentiation, apoptosis, DNA repair and other physiological activities. E3 ubiquitin ligase is the major component of ubiquitinproteasome system, which is responsible for substrate recognition. The abnormal regulation of E3 ubiquitin ligase may cause many diseases such as cancer, Alzheimer's disease and Parkinson's disease. Here, we summarizes the progress of drugs targeting E3 ubiquitin ligase in cancer, Alzheimer's disease, Parkinson's disease, diabetic complications, atherosclerosis, and inflammatory bowel diseases. At present, only a few of small molecule antagonists or agonists targeting E3 ubiquitin ligase are under development. The study of natural products in China is leading the way in the world, and numerous natural products have been identified for pharmacological effects on E3 ubiquitin ligase, which may open up a new avenue for multiple complex diseases.
