Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, the University of Queensland, Brisbane Qld 4072, Australia.
Curr Med Chem. 2020;27(19):3098-3122. doi: 10.2174/0929867325666181001112821.
Low Voltage-Activated (LVA) T-type calcium channels are characterized by transient current and Low Threshold Spikes (LTS) that trigger neuronal firing and oscillatory behavior. Combined with their preferential localization in dendrites and their specific "window current", T-type calcium channels are considered to be key players in signal amplification and synaptic integration. Assisted by the emerging pharmacological tools, the structural determinants of channel gating and kinetics, as well as novel physiological and pathological functions of T-type calcium channels, are being uncovered. In this review, we provide an overview of structural determinants in T-type calcium channels, their involvement in disorders and diseases, the development of novel channel modulators, as well as Structure-Activity Relationship (SAR) studies that lead to rational drug design.
低电压激活 (LVA) T 型钙通道的特点是瞬时电流和低阈值尖峰 (LTS),它们触发神经元放电和振荡行为。T 型钙通道与它们在树突中的优先定位以及它们特定的“窗口电流”相结合,被认为是信号放大和突触整合的关键因素。借助新兴的药理学工具,通道门控和动力学的结构决定因素,以及 T 型钙通道的新的生理和病理功能正在被揭示。在这篇综述中,我们提供了 T 型钙通道结构决定因素的概述,它们在疾病和障碍中的作用,新型通道调节剂的开发,以及导致合理药物设计的结构活性关系 (SAR) 研究。