Ca2+-gramicidin A interactions and blocking effects on the ionic channel

From spectroscopic data (infrared, CD and 13C-NMR) it is shown that Ca2+ interacts with gramicidin A and that a head-to-head gramicidin A dimer can have two Ca2+-binding sites located near the COOH termini. On the basis of this result, we can propose an explanation for the blocking effect of Ca2+ on the transport of alkali metal ions (Cs+ and K+) through gramicidin channels. The binding of Ca2+ is competitive with the alkali metal ion binding; Ca2+ cannot cross the gramicidin channel and its binding in the channel is voltage dependent. From the proposed model, it is possible to account for the influence of the addition of Ca2+ on the single-channel limiting conductance and on the variation of the single-channel current as a function of the voltage in the presence of Cs+ or K+.