Research progress of small molecule proteasome activators
10.16438/j.0513-4870.2021-1549
- VernacularTitle:小分子蛋白酶体激动剂的研究进展
- Author:
Qian YU
1
,
2
;
Yu CAO
1
,
2
;
Hua-jian ZHU
1
,
2
;
Jia-an SHAO
1
,
2
;
Jian-kang ZHANG
1
,
2
Author Information
1. School of Medicine, Zhejiang University City College, Hangzhou 310015, China
2. College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
- Publication Type:Research Article
- Keywords:
proteasome;
activator;
structure-activity relationship;
intrinsically disordered protein;
neurodegenerative disease
- From:
Acta Pharmaceutica Sinica
2022;57(3):605-614
- CountryChina
- Language:Chinese
-
Abstract:
Proteasome controls the degradation of proteins closely related to life activities and plays a key role in the maintenance of protein homeostasis. Proteasome activities decrease with aging, followed by the overwhelming production of damaged proteins which far exceed the protein consumption. Accumulation of these proteins leads to various diseases including neurodegenerative diseases. Therefore, inducing toxic protein degradation is considered as a promising solution for the treatment of these diseases, while increasing the activity of proteasome is considered as an important strategy. However, the research in this field is still in the preliminary stage, and this review will focus on the discussion of the research progress of various small molecule proteasome activators, including research methods, pharmacological effects, structure-activity relationships and the existing problems.
