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Updated: Jul 18, 2026

18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor (SiFA) for Positron Emission Tomography
Published on: January 11, 2020
Fluorine-18 labeling of peptides and proteins
1Nuklearmedizinische Klinik und Poliklinik und Institut für Radiochemie, Technische Universität Müchen, Germany. H.J.Wester@lrz.tum.de
Abstract:
The pool of promising peptides worthy of investigation and evaluation for clinical use is continuously filled from different sources. Driven by the promising results obtained with peptides addressing somatostatin-2 receptor positive (sst2+) neuroendocrine tumours, other peptides targeting further receptor systems are being studied and evaluated. Progress in profiling the density and incidence of peptide hormone receptors in human cancer has initiated and will further promote research on the corresponding peptidic binders. In addition, industrial pharmaceutical research will be another significant source of peptides in the future. A recent prognosis revealed that about 50% of the drugs entering clinical trials in the next years will be peptides. The extensive research activities in genomics and proteomics will point out and quantify new and already known target structures upregulated in specific diseases. Based on the knowledge of their endogenous ligands or via selection of suitable candidates by phage display, suitable peptide ligands for e.g. membrane associated receptors can be identified and thus allow targeting of such binding sites. Thus, bioactive peptides specifically addressing relevant molecular targets are expected to become an important class of tracers, also due to the possibility of bridging imaging with therapeutic approaches. In this brief overview a summary of methods and strategies for the 18F-labeling of peptides and proteins is given.
Insights
Peptides are emerging as crucial drug candidates, with 50% of future clinical trials expected to involve them. Research is advancing peptide-based therapies and diagnostic tracers for various diseases, including cancer.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Peptides are increasingly recognized for their therapeutic potential, particularly in targeting somatostatin-2 receptor-positive neuroendocrine tumors.
- Advancements in understanding peptide hormone receptor expression in cancers are driving research into novel peptide-based therapeutics and diagnostics.
- Peptides are projected to constitute approximately 50% of drugs entering clinical trials in the coming years.
Purpose of the Study:
- To provide an overview of methods and strategies for the 18F-labeling of peptides and proteins.
- To highlight the growing importance of bioactive peptides in disease targeting and molecular imaging.
- To discuss the potential of peptides in bridging diagnostic imaging and therapeutic applications.
Main Methods:
- Review of current research in peptide drug discovery and development.
- Exploration of techniques for identifying peptide ligands, including phage display.
- Summary of methodologies for incorporating fluorine-18 (18F) into peptides and proteins for imaging.
Main Results:
- Peptide hormone receptor profiling in human cancers is accelerating research on targeted peptide binders.
- Genomics and proteomics are identifying new disease-associated molecular targets for peptide-based interventions.
- 18F-labeled peptides show promise as diagnostic tracers and therapeutic agents.
Conclusions:
- Bioactive peptides are poised to become a significant class of molecular imaging tracers and therapeutic agents.
- The development of targeted peptide ligands is crucial for advancing precision medicine.
- 18F-labeling techniques are essential for realizing the full potential of peptides in clinical applications.
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