设计用于定制抑制钙（V）通道的蛋白质。
Engineering proteins for custom inhibition of Ca(V) channels.
作者信息
Xu Xianghua, Colecraft Henry M
机构信息
Department of Physiology and Cellular Biophysics, College of Physicians and Surgeons, Columbia University, New York, New York, USA.
出版信息
Physiology (Bethesda). 2009 Aug;24:210-8. doi: 10.1152/physiol.00010.2009.
Abstract
The influx of Ca(2+) ions through voltage-dependent calcium (Ca(V)) channels links electrical signals to physiological responses in all excitable cells. Not surprisingly, blocking Ca(V) channel activity is a powerful method to regulate the function of excitable cells, and this is exploited for both physiological and therapeutic benefit. Nevertheless, the full potential for Ca(V) channel inhibition is not being realized by currently available small-molecule blockers or second-messenger modulators due to limitations in targeting them either to defined groups of cells in an organism or to distinct subcellular regions within a single cell. Here, we review early efforts to engineer protein molecule blockers of Ca(V) channels to fill this crucial niche. This technology would greatly expand the toolbox available to physiologists studying the biology of excitable cells at the cellular and systems level.
摘要
通过电压依赖性钙（Ca(V)）通道流入的Ca(2+)离子将电信号与所有可兴奋细胞中的生理反应联系起来。毫不奇怪，阻断Ca(V)通道活性是调节可兴奋细胞功能的一种有效方法，并且这一方法已被用于生理和治疗目的。然而，由于目前可用的小分子阻滞剂或第二信使调节剂在将它们靶向生物体中特定的细胞群或单个细胞内不同的亚细胞区域方面存在局限性，Ca(V)通道抑制的全部潜力尚未实现。在此，我们回顾了早期设计Ca(V)通道蛋白分子阻滞剂以填补这一关键空白的努力。这项技术将极大地扩展生理学家在细胞和系统水平研究可兴奋细胞生物学时可用的工具库。
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