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Updated: May 25, 2026

Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions
Published on: January 7, 2019
Peptide-receptor ligands and multivalent approach
Paolo Ruzza1, Anna Marchiani, Nicola Antolini
1Institute of Biomolecular Chemistry of CNR, Padova Unit, via Marzolo 1, 35131 Padova, Italy. paolo.ruzza@unipd.it
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.
Insights
Targeting peptide ligands, overexpressed in tumors, offer promising cancer imaging and therapy. Advances in peptide synthesis and radiolabeling enable development of targeted radiopharmaceuticals for improved cancer treatment.
Area of Science:
- Oncology
- Radiopharmaceutical Chemistry
- Molecular Imaging
Background:
- Overexpressed peptide receptors on human tumors present therapeutic and diagnostic targets.
- Peptide-ligands are attractive for targeted cancer imaging and therapy.
- Radiopharmaceuticals combine bioactive peptides with radionuclides for targeted delivery.
Purpose of the Study:
- To review principal receptor-binding peptides and their tumor cell overexpression.
- To discuss advantages and challenges in developing multivalent peptide-based ligands.
- To summarize design strategies and applications of peptide-based ligands in oncology.
Main Methods:
- Review of scientific literature on receptor-binding peptides.
- Analysis of peptide synthesis, phage display, and combinatorial chemistry techniques.
- Examination of bifunctional chelating agents and radiolabeling methods.
Main Results:
- Identified key receptor-binding peptides overexpressed on various tumor cells.
- Highlighted advancements in peptide-based ligand development through modern synthesis and display technologies.
- Demonstrated the utility of radiolabeled peptides in diagnostic imaging and therapeutic applications.
Conclusions:
- Peptide-ligands are valuable tools for targeted cancer diagnostics and therapeutics.
- Multivalent peptide designs offer enhanced targeting but present development challenges.
- Continued research in peptide chemistry and radiolabeling will advance targeted cancer medicine.
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