Multimerization improves targeting of peptide radio-pharmaceuticals

Curr Pharm Des. 2012;18(17):2501-16. doi: 10.2174/13816128112092501.


Multimerization offers unique kinetic and thermodynamic properties to molecules. Multimeric ligands, characterized by multiple similar or different monomeric molecules tethered together, can bind several receptors simultaneously. Multimerization occurs also in nature. This process can be used to develop molecules with high diagnostic and therapeutic value. By altering parameters as linkers` length and flexibility, scaffold and backbones insertion, and ligands-receptors recognition, it is possible to provide high selectivity and binding affinity. The resultant multimeric ligand has a more favorable binding affinity than corresponding monomeric ligands.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cross-Linking Reagents / chemistry
  • Dimerization
  • Drug Design*
  • Humans
  • Kinetics
  • Ligands
  • Molecular Weight
  • Nanotechnology
  • Peptides / chemistry*
  • Peptides / metabolism
  • Peptides / pharmacology*
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacology*
  • Receptors, Cell Surface / antagonists & inhibitors
  • Receptors, Cell Surface / metabolism
  • Thermodynamics


  • Cross-Linking Reagents
  • Ligands
  • Peptides
  • Radiopharmaceuticals
  • Receptors, Cell Surface