Bioelectricity Laboratory, Department of Physiology and Biophysics, School of Medicine, University of California, Irvine, CA, USA.
Handb Exp Pharmacol. 2021;267:445-480. doi: 10.1007/164_2021_512.
Potassium channels facilitate and regulate physiological processes as diverse as electrical signaling, ion, solute and hormone secretion, fluid homeostasis, hearing, pain sensation, muscular contraction, and the heartbeat. Potassium channels are each formed by either a tetramer or dimer of pore-forming α subunits that co-assemble to create a multimer with a K-selective pore that in most cases is capable of functioning as a discrete unit to pass K ions across the cell membrane. The reality in vivo, however, is that the potassium channel α subunit multimers co-assemble with ancillary subunits to serve specific physiological functions. The ancillary subunits impart specific physiological properties that are often required for a particular activity in vivo; in addition, ancillary subunit interaction often alters the pharmacology of the resultant complex. In this chapter the modes of action of ancillary subunits on K channel physiology and pharmacology are described and categorized into various mechanistic classes.
钾通道促进和调节生理过程,如电信号、离子、溶质和激素分泌、体液平衡、听觉、疼痛感觉、肌肉收缩和心跳。钾通道由形成孔的α亚基的四聚体或二聚体组成,这些亚基共同组装成一个具有 K 选择性孔的多聚体,在大多数情况下,该孔能够作为一个离散的单位将 K 离子穿过细胞膜。然而,在体内的实际情况是,钾通道α亚基多聚体与辅助亚基共同组装,以发挥特定的生理功能。辅助亚基赋予特定的生理特性,这些特性通常是体内特定活动所必需的;此外,辅助亚基的相互作用常常改变所得复合物的药理学。在本章中,描述了辅助亚基对 K 通道生理学和药理学的作用模式,并将其分类为各种机制类别。