离子通道药物研发中的高通量筛选技术

doi:10.5246/jcps.2021.10.066

摘要/Abstract

摘要：

离子通道是极具潜力的药物靶点。近年来, 越来越多的新的离子通道靶标在疾病中被发现, 比如: 疼痛、心血管疾病以及神经系统疾病。尽管离子通道与疾病相关, 并参与多种生理功能, 但它们作为药物靶点被开发的还远远不够。这在很大程度上是由于缺乏可以同时确保数据质量和高通量的筛选技术造成的。然而, 在过去的几十年里, 越来越多的检测方法和技术迅速发展。在本文中我们将概述近年来在离子通道药物发现中应用的高通量筛选技术。

关键词: 离子通道, 药物研发, 高通量筛选

Abstract:

Ion channels are attractive targets for drug discovery as an increasing number of new ion channel targets have been uncovered in diseases, such as pain, cardiovascular disease, and neurological disorders. Despite their relevance in diseases and the variety of physiological functions they are involved in, ion channels still remain underexploited as drug targets. This, to a large extent, is attributed to the absence of screening technologies that ensure both the quality and the throughput of data. However, an increasing number of assays and technologies have evolved rapidly in the past decades. In this review, we summarized the currently available high-throughput screening technologies in ion channel drug discovery.

Key words: Ion channels, Drug discovery, High-throughput screening

Supporting:

段桂芳, 徐波, 袁霞, 宋书香. 离子通道药物研发中的高通量筛选技术[J]. 中国药学(英文版), 2021, 30(10): 785-793.

Guifang Duan, Bo Xu, Xia Yuan, Shuxiang Song. High-throughput screening technologies for ion channel drug discovery[J]. Journal of Chinese Pharmaceutical Sciences, 2021, 30(10): 785-793.

图/表 4

Figure 1. HTS technologies for ion channel drug discovery.

Figure 2. Schematic illustrations of ion flux assay using AAS.

Figure 3. Schematic illustrations of FRET-based assay.

Figure 4. Schematic illustrations of patch-clamp.

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