由于电压敏感钠通道（VGSC）与多种疾病有着密切的联系，因此它是相关多肽药物开发的重要靶点，但是这类多肽药物的开发过程却十分缓慢和昂贵，其中一个最主要的原因就是活性多肽的有效鉴定。为了加速这一过程，本项目拟依托酵母双杂交筛选平台以及具有抑制剂半胱氨酸结结构（ICK模体）的随机多肽文库，以高通量的方式来初步筛选出潜在的能够与人源电压敏感钠通道亚型（hNav1.5和hNav1.7）相互作用的多肽，最后利用多肽细胞膜上展示技术与电压钳实验快速地进一步确认多肽活性，并对其进行相关电生理研究。本项目的开展不但能够获取若干具有潜在药用开发价值的多肽，更重要的是能发展并完善一种加速获得电压敏感钠通道相互作用多肽的方法，为相关药物开发提供有力支撑。

Voltage-gated sodium channel (VGSC) is linked to many diseases and it is considered as an important target for the peptide drug development and design. However, the procedure of the research and development (R&D) of this kind of peptide is very slowly and expensive. One main rate-determining step is hard to identify relative bioactive peptides efficiently, which is costly and time-consuming. Our project, using Yeast-Two-Hybrid assays, is set out to high throughput screening the random peptide library possessing inhibitor cysteine knot motif (ICK motif) for identifying the peptides which might be interacting with human VGSC subtypes (hNav1.5 or hNav1.7). The identified peptides will be further hetero-expressed and tethered on the surface of Xenopus laevis oocytes to analyze its’ electrophysiological characterizations and interacting sites using the two-electrode voltage clamp assays. In this project, we will not only to obtain several potential medicinal value peptides, moreover, we can also develop and refine an effective solution for accelerating identification VGSC interacting peptides which can greatly benefit the R&D of this kind of peptide drugs.