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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Peptide-Receptor Ligands and Multivalent Approach

Author(s): Paolo Ruzza, Anna Marchiani, Nicola Antolini and Andrea Calderan

Volume 12, Issue 5, 2012

Page: [416 - 427] Pages: 12

DOI: 10.2174/187152012800617849

Price: $65


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.

Keywords: Peptide-receptors, Multivalent approach, Tumour imaging, Cholecystokinin, Metallosilicates, Somatostatin, Vasoactive Intestinal Peptide, Melanocortin Peptides, Bombesin, radiopeptides

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