[Advances in the development of transient receptor potential melastatin 2 channel inhibitors].

Q2 Medicine
Shiyao Chen, Yanping Luo, Peilin Yu, Xiaomin Yue, Wei Yang
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引用次数: 0

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.

TRPM2通道抑制剂的研究进展。
特异性瞬时受体电位美拉他汀2(TRPM2)通道抑制剂的研究可以加深我们对相关疾病病理机制的认识,发现新的、有效的治疗药物靶点。TRPM2通道抑制剂的发展大致可分为四类,各具有鲜明的特点:对同源离子通道调节剂进行再利用和结构修饰,制备出具有强抑制作用的多种TRPM2通道抑制剂;TRPM2通道抑制剂基于通道门控机制开发,具有高特异性;通过高通量筛选开发出具有新型化学结构的抑制剂;从天然抗氧化剂中开发的抑制剂具有更高的安全性。近年来,计算机辅助药物设计的应用显著加速了TRPM2通道抑制剂的发展。目前已经发现了ZA18、A1和D9等几种有前景的化合物,预计未来还会发现更有效、更有选择性的TRPM2通道抑制剂支架。本文综述了TRPM2通道抑制剂的研究进展,旨在为TRPM2通道抑制剂的进一步研究和临床应用提供参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
3.80
自引率
0.00%
发文量
67
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