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Current Medicinal Chemistry

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ISSN (Online): 1875-533X

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Review Article

Radiolabeled Protein-inhibitor Peptides with Rapid Clinical Translation towards Imaging and Therapy

Author(s): Guillermina Ferro-Flores*, Blanca Ocampo-García, Myrna Luna-Gutiérrez, Clara Santos-Cuevas, Nallely Jiménez-Mancilla, Erika Azorín-Vega and Laura Meléndez-Alafort

Volume 27, Issue 41, 2020

Page: [7032 - 7047] Pages: 16

DOI: 10.2174/0929867327666191223121211

Price: $65

Abstract

Protein interactions are the basis for the biological functioning of human beings. However, many of these interactions are also responsible for diseases, including cancer. Synthetic inhibitors of protein interactions based on small molecules are widely investigated in medicinal chemistry. The development of radiolabeled protein-inhibitor peptides for molecular imaging and targeted therapy with quickstep towards clinical translation is an interesting and active research field in the radiopharmaceutical sciences. In this article, recent achievements concerning the design, translational research and theranostic applications of structurally-modified small radiopeptides, such as prostate-specific membrane antigen (PSMA) inhibitors, fibroblast activation protein (FAP) inhibitors and antagonists of chemokine-4 receptor ligands (CXCR-4-L), with high affinity for cancer-associated target proteins, are reviewed and discussed.

Keywords: Radiolabeled peptides, inhibitor peptides, translational radiopeptides, PSMA, FAP, CXCR-4.

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