Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex


Peptide-Receptor Ligands and Multivalent Approach

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


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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Article Details

Year: 2012
Page: [416 - 427]
Pages: 12
DOI: 10.2174/187152012800617849
Price: $58