Laboratório de Biofísica Teórica e Computacional, Departamento de Biologia Celular, Universidade de Brasília, DF, Brasília, Brazil.
Biochemistry. 2013 Mar 5;52(9):1501-13. doi: 10.1021/bi3013017. Epub 2013 Feb 12.
Because of their remarkable roles in electrical cell signaling, voltage-gated cation channels (VGCCs) have been the subject of intense investigations and debate for more than 50 years. Ultimately, the prospective implications of such studies have an impact on our understanding of the molecular properties of VGCCs involved in consciousness, anesthesia, and diseases, to mention a few. The following review aims to summarize our current knowledge of activation of VGCCs by highlighting major methodological innovations in the field and the breakthroughs they allowed. Focusing mainly on insights gained through computer simulations, while acknowledging important experimental findings, we hope to inspire experimentalists to benefit from these approaches in the generation of hypotheses and design of experiments. Also, we outline major future challenges for the field, such as channel modulation, lesser-known receptors, and molecular origins of channel dysfunctions.
由于其在电细胞信号传递中的显著作用，电压门控阳离子通道（VGCC）已经成为 50 多年来激烈研究和争论的主题。最终，这些研究的预期影响对我们理解涉及意识、麻醉和疾病等方面的 VGCC 的分子特性产生了影响。以下综述旨在通过强调该领域的主要方法创新及其所允许的突破，总结我们目前对 VGCC 激活的认识。主要关注通过计算机模拟获得的见解，同时承认重要的实验发现，我们希望启发实验者从这些方法中受益，以提出假设和设计实验。此外，我们还概述了该领域的主要未来挑战，如通道调节、鲜为人知的受体以及通道功能障碍的分子起源。
