Criteria for the design and biological characterization of radiolabeled peptide-based pharmaceuticals

BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
Ettore BenedettiL Aloj

Abstract

Radiolabeled peptide-based formulations are being evaluated for their application in oncological imaging and therapy using nuclear medicine techniques. A major breakthrough in the field was the discovery and identification of the G-protein coupled receptor superfamily that are overexpressed in a variety of human cancers. These receptors act as targets for endogenous compounds, often of peptidic nature, which can be radiolabeled and, therefore, could potentially be utilized as radiopharmaceuticals. This general strategy has proven successful for application in humans in only a few cases thus far. However, the use of more sophisticated structural methodology to enhance our understanding of the interactions between the receptor and the endogenous peptide or its analogs, and a more efficient preclinical evaluation process, may help to single out the most promising compounds for further development and eventual use in the clinical application of radiopharmaceuticals. This review analyzes current methods of approaching these key points. The rational process for developing peptide-based radiopharmaceuticals is presented, from the structural analysis of the peptide-receptor interaction for the identification and modeling of the peptide...Continue Reading

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Citations

Jan 22, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Zi-Bo LiXiaoyuan Chen
Mar 17, 2010·Amino Acids·Yongjun Yan, Xiaoyuan Chen
Jan 28, 2010·Biochemistry·Seulki LeeXiaoyuan Chen
Mar 17, 2010·Chemical Reviews·Seulki LeeXiaoyuan Chen
Jul 17, 2008·Biological Chemistry·Hannu KoistinenUlf-Håkan Stenman
Aug 12, 2015·Molecular BioSystems·Marian VincenziDiego Tesauro
Apr 20, 2013·Chemical Communications : Chem Comm·Caterina F Ramogida, Chris Orvig
Feb 22, 2008·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Zi-Bo LiXiaoyuan Chen

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