Peptides, multimers and polymers.

ABSTRACT

Due to their favorable properties and pharmacokinetics, peptides are often regarded as "agents of choice" for imaging and radiotherapy. Chemical strategies have been developed that allow their site specific labeling with various radionuclides for PET and SPECT, without compromising their biological integrity. Together with the overexpression of a wide range of peptide receptors and binding sites on tumor cells or matrix components, this class of compounds offers multiple imaging applications. Furthermore, radiolabeled peptides have great potential as carrier molecules for site-specific delivery of other signalling units, such as fluorescent moieties, cyctotoxic compounds or metals for magnetic resonance imaging. In addition, great efforts have been made to exploit the favorable characteristics of peptides for the development of larger constructs, such as multimeric ligands, polymer-peptide conjugates and "peptide-coated" liposomes and nanoparticles. Some peptides have already entered clinical routine application; some are currently being evaluated in clinical studies. However, a variety of peptides is still "waiting" to enter the imaging arena. This chapter presents a brief overview of the highly active field of peptide radiopharmaceuticals and the future potential of multimeric and polymeric peptide constructs.