Potassium Channels: Structures, Diseases, and Modulators

• Published in: Chemical biology & drug design 2014-01, Vol.83 (1), p.1-26
• Main Authors: Tian, Chuan, Zhu, Ruixin, Zhu, Lixin, Qiu, Tianyi, Cao, Zhiwei, Kang, Tingguo
• Format: Article
• Language: English
• Subjects: Biological Products - chemistry; Biological Products - pharmacokinetics; disease; Half-Life; Heart Diseases - metabolism; Heart Diseases - pathology; Humans; modulator; Molecular Dynamics Simulation; Neurodegenerative Diseases - metabolism; Neurodegenerative Diseases - pathology; potassium channel; Potassium Channel Blockers - chemistry; Potassium Channel Blockers - pharmacokinetics; Potassium Channels - chemistry; Potassium Channels - classification; Potassium Channels - metabolism; Protein Structure, Tertiary; structure
• ISSN: 1747-0277; 1747-0285
• DOI: 10.1111/cbdd.12237

Potassium channels participate in many critical biological functions and play important roles in a variety of diseases. In recent years, many significant discoveries have been made which motivate us to review these achievements. The focus of our review is mainly on three aspects. Firstly, we try to summarize the latest developments in structure determinants and regulation mechanism of all types of potassium channels. Secondly, we review some diseases induced by or related to these channels. Thirdly, both qualitative and quantitative approaches are utilized to analyze structural features of modulators of potassium channels. Our analyses further prove that modulators possess some certain natural‐product scaffolds. And pharmacokinetic parameters are important properties for organic molecules. Besides, with in silico methods, some features that can be used to differentiate modulators are derived. There is no doubt that all these studies on potassium channels as possible pharmaceutical targets will facilitate future translational research. All the strategies developed in this review could be extended to studies on other ion channels and proteins as well. Three aspects including structures, diseases and modulators are mainly discussed in this review. The latest developments in structure determinants and regulation mechanism of all types of potassium channels are summarized. Diseases related to potassium channels are reviewed. Both qualitative and quantitative analyses are made on modulators. All these studies on potassium channels as possible pharmaceutical targets will facilitate translational research in the future.