Vascular Biology Research Centre, Molecular and Clinical Sciences Institute, St George's, University of London, London, SW17 0RE, United Kingdom; email:
Annu Rev Pharmacol Toxicol. 2018 Jan 6;58:625-648. doi: 10.1146/annurev-pharmtox-010617-052912. Epub 2017 Oct 6.
K7 channels are voltage-gated potassium channels encoded by KCNQ genes that have a considerable physiological impact in many cell types. This reliance upon K7 channels for normal cellular function, as well as the existence of hereditary disorders caused by mutations to KCNQ genes, means that pharmacological targeting of these channels has broad appeal. Consequently, a plethora of chemical entities that modulate K7 channel activity have been developed. Moreover, K7 channels are influenced by many disparate intracellular mediators and trafficking processes, making upstream targeting an appealing prospect for therapeutic development. This review covers the main characteristics of these multifunctional and versatile channels with the aim of providing insight into the therapeutic value of targeting these channels.
K7 通道是由 KCNQ 基因编码的电压门控钾通道，在许多细胞类型中具有重要的生理影响。这种对 K7 通道正常细胞功能的依赖，以及由 KCNQ 基因突变引起的遗传性疾病的存在，意味着这些通道的药理学靶向具有广泛的吸引力。因此，已经开发出了大量调节 K7 通道活性的化学实体。此外，K7 通道受到许多不同的细胞内介质和运输过程的影响，使得上游靶向成为治疗开发的一个有吸引力的前景。本综述涵盖了这些多功能和通用通道的主要特征，旨在为靶向这些通道的治疗价值提供深入了解。
