Abstract
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
Anti-Cancer Agents in Medicinal Chemistry
Title:Peptide-Receptor Ligands and Multivalent Approach
Volume: 12 Issue: 5
Author(s): Paolo Ruzza, Anna Marchiani, Nicola Antolini and Andrea Calderan
Affiliation:
Keywords: Peptide-receptors, Multivalent approach, Tumour imaging, Cholecystokinin, Metallosilicates, Somatostatin, Vasoactive Intestinal Peptide, Melanocortin Peptides, Bombesin, radiopeptides
Abstract: 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.
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Cite this article as:
Ruzza Paolo, Marchiani Anna, Antolini Nicola and Calderan Andrea, Peptide-Receptor Ligands and Multivalent Approach, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (5) . https://dx.doi.org/10.2174/187152012800617849
DOI https://dx.doi.org/10.2174/187152012800617849 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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