A new saccharide-directed chemical modification method toward a protein surface was developed. Hydrophobic guests such as Dansyl-SE were effectively incorporated by the cyclophane (1) having terminal glucose moieties. The amine-coupling fluorescent dye was carried from the aqueous phase to the glucoside-binding site of Con A by 1 and reacted at the proximal binding site. The modified Con A acts as a fluorescent saccharide biosensor.