The use of supramolecular interactions in catalysis has undergone major growth in the last decade and has contributed to the major advances achieved in the field of enantioselective catalysis. Of the various approaches that use supramolecular interactions in enantioselective catalysis, this article highlights different supramolecular strategies to generate a set of enantiopure ligands (or enantioselective catalysts) that retain the majority of the backbone’s structural features, yet at the same time incorporate subtle changes at its active site that depend on the structural characteristics of the regulation agent (RA) employed.