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Advances in the development of novel E3 ubiquitin ligase ligands
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Chen-xi WANG, Yang LU, Xiao-wu DONG*, Jin-xin CHE*
Acta Pharmaceutica Sinica | 2024, 59(11) : 2926 - 2940
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Acta Pharmaceutica Sinica | 2024, 59(11): 2926-2940
Advances in the development of novel E3 ubiquitin ligase ligands
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Chen-xi WANG, Yang LU, Xiao-wu DONG*, Jin-xin CHE*
Affiliations
  • Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310000, China
Published: 2024-11-12 doi: 10.16438/j.0513-4870.2024-0093
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The ubiquitin-proteasome system (UPS) is responsible for protein degradation in both normal and pathological states. E3 ligases selectively attach ubiquitin to specific substrates, which is essential for regulating cellular homeostasis. The function of E3 ligases has been associated with a variety of diseases, such as cancer and cardiovascular disease. The discovery of E3 ligands can help regulate E3 ligases, thus expanding new ideas for disease treatment. Targeted protein degradation (TPD) drugs, including proteolysis targeting chimera (PROTAC), have become increasingly popular in recent years due to their dependence on E3 ligands. In this paper, we review the discovery techniques of E3 ligands, including activity-based protein mapping, fragment-based drug discovery, and library-based methods, and briefly introduce the protein interaction detection techniques involved in the ligand discovery techniques, in the hope of providing certain ideas for the future discovery of E3 ligands as well as the treatment of diseases.

ubiquitin-proteasome system  /  ligand discovery  /  E3 ubiquitin ligase  /  interaction
Chen-xi WANG, Yang LU, Xiao-wu DONG, Jin-xin CHE. Advances in the development of novel E3 ubiquitin ligase ligands[J]. Acta Pharmaceutica Sinica, 2024 , 59 (11) : 2926 -2940 . DOI: 10.16438/j.0513-4870.2024-0093
Year 2024 volume 59 Issue 11
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doi: 10.16438/j.0513-4870.2024-0093
  • Receive Date:2024-01-29
  • Online Date:2025-11-24
  • Published:2024-11-12
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  • Received:2024-01-29
  • Revised:2024-05-02
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    Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310000, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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