Progress in the synthesis of membrane-bound ion channels is reviewed. Important results from several groups are highlighted and contributions from the authors’ group are summarized. Topics covered include synthetic approaches towards oligo-THF amino acids, oligopyrrolidines and gramicidin hybrid channels. Points of interest are the importance of self-assembly systems, the functional analysis (ion selectivity, gating, asymmetric insertion and asymmetric function) and the structural characterization of the channel. 1 Introduction 2 Polyether-Containing Ion Channels 3 Peptide β-Helix as Ion Channel Motif 4 Ion Selectivity in Synthetic Ion Channels 5 THF-Gramicidin Hybrid Channels and Asymmetric Insertion into the Membrane 6 Minigramicidins: Hydrophobic Match/Mismatch with the Membrane and a Conformational Switch 7 Synthetic Ion Channels by Self-Assembly of the Pore 8 Outlook