Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, 229 Taibai Road, Xi'an 710069, China.
Biomedicine Key Laboratory of Shaanxi Province, School of Pharmacy, Northwest University, 229 Taibai Road, Xi'an 710069, China.
Biomolecules. 2019 Dec 19;10(1):10. doi: 10.3390/biom10010010.
The voltage-gated potassium channel Kv1.5, which mediates the cardiac ultra-rapid delayed-rectifier (I) current in human cells, has a crucial role in atrial fibrillation. Therefore, the design of selective Kv1.5 modulators is essential for the treatment of pathophysiological conditions involving Kv1.5 activity. This review summarizes the progress of molecular structures and the functionality of different types of Kv1.5 modulators, with a focus on clinical cardiovascular drugs and a number of active natural products, through a summarization of 96 compounds currently widely used. Furthermore, we also discuss the contributions of Kv1.5 and the regulation of the structure-activity relationship (SAR) of synthetic Kv1.5 inhibitors in human pathophysiology. SAR analysis is regarded as a useful strategy in structural elucidation, as it relates to the characteristics that improve compounds targeting Kv1.5. Herein, we present previous studies regarding the structural, pharmacological, and SAR information of the Kv1.5 modulator, through which we can assist in identifying and designing potent and specific Kv1.5 inhibitors in the treatment of diseases involving Kv1.5 activity.
电压门控钾通道 Kv1.5 在人类细胞中介导心脏超快延迟整流（I）电流，在心房颤动中起关键作用。因此，设计选择性 Kv1.5 调节剂对于治疗涉及 Kv1.5 活性的病理生理状况至关重要。本综述通过总结目前广泛使用的 96 种化合物，总结了不同类型 Kv1.5 调节剂的分子结构和功能的进展，重点介绍了临床心血管药物和一些活性天然产物。此外，我们还讨论了 Kv1.5 的作用以及合成 Kv1.5 抑制剂的结构-活性关系（SAR）在人类病理生理学中的调节。SAR 分析被认为是结构阐明的有用策略，因为它与改善针对 Kv1.5 的化合物的特征有关。在此，我们介绍了 Kv1.5 调节剂的结构、药理学和 SAR 信息的先前研究，通过这些研究，我们可以协助识别和设计针对 Kv1.5 活性的疾病的有效和特异性 Kv1.5 抑制剂。
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