GtoPdb v.2023.1中的电压门控钾通道(Kv)

B. Attali, K. Chandy, M. Giese, S. Grissmer, G. Gutman, L. Jan, M. Lazdunski, D. Mckinnon, J. Nerbonne, L. Pardo, Gail A. Robertson, B. Rudy, M. Sanguinetti, W. Stühmer, J. Trimmer, Xiaoliang Wang
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摘要

6TM K通道家族包括电压门控KV亚家族、EAG亚家族(包括hERG通道)、Ca2+激活的Slo亚家族(实际上与7TM一起,称为BK)和Ca2+激活的SK亚家族。这些通道具有成孔α亚基,由相同亚基(同质)或不同亚基(异质)的四聚体组成。异质通道只能在亚族中形成(例如Kv1.1与Kv1.2;Kv7.2与Kv7.3)。药理学在很大程度上反映了功能通道的亚基组成。Kv7通道skv7.1 - kv7.5 (KCNQ1-5) K+通道是电压门控的K+通道,在神经元、肌肉细胞和上皮细胞中起主要作用,它们是生理上重要的K+电流的基础,如神经元m电流和心脏ik。所有五个KCNQ基因的遗传缺陷导致人类兴奋性障碍,包括癫痫、自闭症谱系障碍、心律失常和耳聋。由于最近对人类kcnq编码蛋白的结构和功能的了解,这些通道越来越多地被用作治疗疾病的药物靶点[326,2,767]。
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Voltage-gated potassium channels (Kv) in GtoPdb v.2023.1
The 6TM family of K channels comprises the voltage-gated KV subfamilies, the EAG subfamily (which includes hERG channels), the Ca2+-activated Slo subfamily (actually with 7TM, termed BK) and the Ca2+-activated SK subfamily. These channels possess a pore-forming α subunit that comprise tetramers of identical subunits (homomeric) or of different subunits (heteromeric). Heteromeric channels can only be formed within subfamilies (e.g. Kv1.1 with Kv1.2; Kv7.2 with Kv7.3). The pharmacology largely reflects the subunit composition of the functional channel.Kv7 channelsKv7.1-Kv7.5 (KCNQ1-5) K+ channels are voltage-gated K+ channels with major roles in neurons, muscle cells and epithelia where they underlie physiologically important K+ currents, such as the neuronal M-current and the cardiac IKs. Genetic deficiencies in all five KCNQ genes result in human excitability disorders, including epilepsy, autism spectrum disorders, cardiac arrhythmias and deafness. Thanks to the recent knowledge of the structure and function of human KCNQ-encoded proteins, these channels are increasingly used as drug targets for treating diseases [326, 2, 767].
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