Synthetic, ion-conducting transmembrane channels

ORGN 219

G. W. Gokel, Bioorganic Chemistry Program and Department of Molecular Biology & Pharmacology, Bioorganic Chemistry Program and Department of Molecular Biology & Pharmacology, Washington University School of Medicine, 660 S. Euclid Ave., Campus Box 8103, St. Louis, MO 63110
Macrocyclic polyether compounds are excellent cation binders and their complexation behavior has been extensively studied during three decades. We have incorporated macrocycles into structures that we have developed for use as model cation-conducting transmembrane channels. These compounds transport H+, Na+, and K+ through phospholipid membranes. Sodium transport has been assessed by dynamic 23Na-NMR methods and proton flux has been measured by fluorescence techniques. Sodium and potassium fluxes have been determined in certain cases by bilayer clamp methods in phospholipid bilayers. Hydraphile channels are currently thought to form water- and sodium-filled pores through the bilayer. Chloride selectivity represents a second goal and challenge of the synthetic ion channel project. Results describing the design, synthesis, and characterization of an anion-selective channel will also be presented. In this case, the synthetic systems involves an amphiphilic heptapeptide.