Peptide-Receptor Ligands and Multivalent Approach

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

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Peptide-Receptor Ligands and Multivalent Approach

Anti-Cancer Agents in Medicinal Chemistry, 12(5): 416-427.

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

Affiliation: Institute of Biomolecular Chemistry of CNR, Padova Unit, via Marzolo 1, 35131 Padova, Italy.


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.


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

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Article Details

Volume: 12
Issue Number: 5
First Page: 416
Last Page: 427
Page Count: 12
DOI: 10.2174/187152012800617849
Price: $58

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