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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Multimerization Improves Targeting of Peptide Radio-Pharmaceuticals

Author(s): Giuseppe Carlucci, Hildo J.K. Ananias, Zilin Yu, Christophe Van de Wiele, Rudi A. Dierckx, Igle J. de Jong and Philip H. Elsinga

Volume 18 , Issue 17 , 2012

Page: [2501 - 2516] Pages: 16

DOI: 10.2174/13816128112092501

Price: $65

Abstract

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.

Keywords: Multimerization, binding, avidity, cooperativity, valency, ligand design, nuclear imaging, nanotechnology


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