Advances in the development of transient receptor potential melastatin 2 channel inhibitors.
10.3724/zdxbyxb-2024-0586
- Author:
Shiyao CHEN
1
;
Yanping LUO
2
;
Peilin YU
3
;
Xiaomin YUE
4
;
Wei YANG
5
Author Information
1. Department of Biophysics, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China. 22260507@zju.edu.cn.
2. Department of Biophysics, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China.
3. Department of Toxicology, School of Public Health, Zhejiang University School of Medicine , Hangzhou 310058, China.
4. Department of Biophysics, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China. yuexiaomin@zju.edu.cn.
5. Department of Biophysics, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China. yangwei@zju.edu.cn.
- Publication Type:English Abstract
- Keywords:
Computer-aided drug design;
High-throughput screening;
Inhibitors;
Natural antioxidants;
Oxidative stress;
Review;
Structural modification;
Transient receptor potential melastatin 2
- MeSH:
TRPM Cation Channels/antagonists & inhibitors*;
Humans;
Drug Design
- From:
Journal of Zhejiang University. Medical sciences
2025;54(1):120-130
- CountryChina
- Language:Chinese
-
Abstract:
Studies on specific transient receptor potential melastatin 2 (TRPM2) channel inhibitors can deepen our understanding of the pathological mechanism of related diseases, and allow discovery of novel, effective targets and drugs for therapy. The development of TRPM2 channel inhibitors can be broadly classified into four categories with distinct characteristics: reutilization and structural modification of homologous ion channel modulators to produce a diverse array of TRPM2 channel inhibitors with strong inhibitory effects; TRPM2 channel inhibitors based on channel gating mechanism with high specificity; inhibitors identified through high-throughput screening with novel chemical structures; inhibitors developed from natural antioxidants with higher safety. In recent years, the application of computer-aided drug design has significantly accelerated the development of TRPM2 channel inhibitors. Several promising compounds such as ZA18, A1 and D9 have been discovered, and it is expected that more potent and selective TRPM2 channel inhibitor scaffolds will be discovered in the future. This article reviews the advances on the studies of TRPM2 channel inhibitors, aiming to provide insights for further research and clinical application of TRPM2 channel inhibitors.
