Multivalent ligand: design principle for targeted therapeutic delivery approach

Multivalent interactions of biological molecules play an important role in many biochemical events. A multivalent ligand comprises of multiple copies of ligands conjugated to scaffolds, allowing the simultaneous binding of multivalent ligands to multiple binding sites or receptors. Many research groups have successfully designed and synthesized multivalent ligands to increase the binding affinity, avidity and specificity of the ligand to the receptor. A multimeric ligand is a promising option for the specific treatment of diseases. In this review, the factors affecting multivalent interactions, including the size and shape of the ligand, geometry and an arrangement of ligands on the scaffold, linker length, thermodynamic, and kinetics of the interactions are discussed. Examples of the multivalent ligand applications for therapeutic delivery are also summarized.