Ligand/receptor interactions--the influence of the microenvironment on macroscopic properties. Electrostatic...

The heterogeneous environment in which ligand/receptor interactions occur often leads to complex binding behaviour. We consider here the ligand/membrane interaction, emphasizing the possibilities of electrostatic modulation of the overall binding characteristics. The binding of Substance P to neutral or negatively charged planar lipid bilayers was monitored using the capacitance minimization technique. The electrostatic attraction to the charged bilayer potentiates the interaction by more than two orders of magnitude and leads to a nonlinearity in the Scatchard plot of bound vs. bulk concentrations. The Boltzmann accumulation factor, along with the direct measurement of the surface potential, provides an easy explanation of the effect. The general importance of electrostatic accumulation (or repulsion) at surfaces is discussed and the concept applied to examples from the literature.