Catterall W A, Ray R, Morrow C S
Proc Natl Acad Sci U S A. 1976 Aug;73(8):2682-6. doi: 10.1073/pnas.73.8.2682.
Depolarization of neuroblastoma cells causes a 70-fold increase in the apparent dissociation constant KD for scorpion toxin enhancement of activation of the action potential Na+ ionophore by veratridine and a large increase in the rate of reversal of scorpion toxin action. Depolarization also inhibits binding of 125I-labeled scorpion toxin to a small number of saturable binding sites on electrically excitable neuroblastoma cells and increases the rate of dissociation of scorpion toxin from these sites. The results suggest that scorpion toxin binds to a regulatory component of the action potential Na+ ionophore whose conformation changes on depolarization.
神经母细胞瘤细胞的去极化导致蝎毒素增强藜芦碱激活动作电位钠离子载体作用的表观解离常数KD增加70倍,且蝎毒素作用的逆转速率大幅提高。去极化还抑制125I标记的蝎毒素与电可兴奋神经母细胞瘤细胞上少量可饱和结合位点的结合,并增加蝎毒素从这些位点的解离速率。结果表明,蝎毒素与动作电位钠离子载体的一个调节成分结合,该成分的构象在去极化时发生变化。