Multivalency is a common phenomenon in nature to increase affinity and specifity of receptor-ligand interactions, especially on the cell surface. Chemists have tried to make use of multivalent interactions in different context and have synthesized a number of scaffolds for the assembly of multivalent receptor ligands [ 1 ]. We have developed tetrahedral, rigid scaffolds based on adamantane for conjugation to multiple cell surface binders via amide bonds. The resulting novel multivalent conjugates 1 were designed for an efficient interaction with cell surface epitopes and are miniaturized analogs of natural systems like virus particles, resembling their globular shape and a tripodal arrangment of binding ligands. This rigid tripodal geometry is an ideal recognition motif for cell surface receptors.
展开▼
