McCleskey E W, Fox A P, Feldman D H, Cruz L J, Olivera B M, Tsien R W, Yoshikami D
Proc Natl Acad Sci U S A. 1987 Jun;84(12):4327-31. doi: 10.1073/pnas.84.12.4327.
Blockade of Ca2+ channels by omega-conotoxin GVIA, a 27 amino acid peptide from the venom of the marine snail Conus geographus, was investigated with patch-clamp recordings of whole-cell and unitary currents in a variety of cell types. In dorsal root ganglion neurons, the toxin produces persistent block of L- and N-type Ca2+ channels but only transiently inhibits T-type channels. Its actions appear to be neuron-specific, since it blocks high-threshold Ca2+ channels in sensory, sympathetic, and hippocampal neurons of vertebrates but not in cardiac, skeletal, or smooth muscle cells. Block occurs through direct interaction of the toxin with an external site closely associated with the Ca2+ channel, without apparent involvement of a second messenger or dependence on channel gating. The tissue and channel-type specificity and the directness and slow reversibility of the block are features that favor use of omega-conotoxin as a tool for purifying particular neuronal Ca2+ channels and defining their physiological function.
使用膜片钳记录多种细胞类型中的全细胞电流和单通道电流,研究了来自海洋蜗牛地纹芋螺毒液的一种27个氨基酸的肽——ω-芋螺毒素GVIA对Ca2+通道的阻断作用。在背根神经节神经元中,该毒素对L型和N型Ca2+通道产生持续性阻断,但仅短暂抑制T型通道。其作用似乎具有神经元特异性,因为它能阻断脊椎动物感觉神经元、交感神经元和海马神经元中的高阈值Ca2+通道,但对心肌细胞、骨骼肌细胞或平滑肌细胞无此作用。阻断是通过毒素与Ca2+通道紧密相关的外部位点直接相互作用而发生的,显然没有第二信使的参与,也不依赖于通道门控。该毒素的组织和通道类型特异性以及阻断的直接性和缓慢可逆性,使其成为纯化特定神经元Ca2+通道并确定其生理功能的有用工具。