Peptide-receptor ligands and multivalent approach.

Paolo Ruzza, Anna Marchiani, Nicola Antolini, Andrea Calderan

Institute of Biomolecular Chemistry of CNR, Padova Unit, via Marzolo 1, 35131 Padova, Italy. paolo.ruzza@unipd.it

Anti-cancer agents in medicinal chemistry 2012 Jun

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The overexpression of peptide receptors in human tumours makes peptide-ligands attractive agents for the development of specific diagnostic imaging and/or therapy of cancers. Solid-phase peptide synthesis, modern phage display technology and combinatorial peptide chemistry have profoundly affected the pool of available targeting peptides for efficient and specific delivery of imaging or therapeutic label molecules. Additionally, the availability of a wide range of bifunctional chelating agents for the radiolabelling of bioactive peptides with radionuclides has produced a wide variety of useful radiopharmaceutical molecules. This review article examines the principal receptors-binding peptides and their overexpression on tumour cells. We discuss the advantage and the challenges in developing multivalent peptide-based ligands summarising their design strategies and applications.

Citation

Paolo Ruzza, Anna Marchiani, Nicola Antolini, Andrea Calderan. Peptide-receptor ligands and multivalent approach. Anti-cancer agents in medicinal chemistry. 2012 Jun;12(5):416-27