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Related Experiment Video

Updated: Nov 5, 2025

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging

Published on: February 3, 2015

Ligand engineering for theranostic applications.

Annette Altmann¹, Clemens Kratochwil², Frederik Giesel²

¹Department of Nuclear Medicine, University Hospital Heidelberg, Germany; Clinical Cooperation Unit Nuclear Medicine, German Cancer Research Center (DKFZ), Heidelberg, Germany.

Current Opinion in Chemical Biology

|May 18, 2021

Summary

This summary is machine-generated.

New radiopharmaceuticals offer improved targeted cancer therapy. Researchers identified fibroblast activation protein inhibitors (FAPI) and alpha-v-beta-6 integrin-binding peptides for precise imaging and treatment of epithelial tumors.

Keywords:

FAPI Fibroblast activation protein Imaging PET SPECT Theranostics

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Published on: January 29, 2019

Area of Science:

Oncology
Biotechnology
Radiopharmaceutical Science

Background:

Targeted cancer therapy presents a promising alternative to traditional chemotherapy and radiotherapy.
Advancements in biotechnology enhance the development of novel radiopharmaceuticals for precise imaging and therapy of epithelial tumors.

Purpose of the Study:

To identify and validate novel radiopharmaceuticals for targeted cancer therapy.
To develop fibroblast activation protein inhibitors (FAPI) and alpha-v-beta-6 integrin-binding peptides for diagnostic imaging and endoradiotherapy.

Main Methods:

Rational design of quinoline-based fibroblast activation protein inhibitors (FAPI).
High-throughput screening of a sunflower trypsin inhibitor 1-based peptide library.
Identification of a novel alpha-v-beta-6 integrin-binding peptide (SFITGv6).

Main Results:

Several FAPI derivatives were identified.
A novel alpha-v-beta-6 integrin-binding peptide, SFITGv6, was discovered.
FAPI and SFITGv6 show potential as radiopharmaceuticals.

Conclusions:

FAPI and SFITGv6 are effective radiopharmaceuticals for targeting FAP- and alpha-v-beta-6 integrin-expressing epithelial tumors, respectively.
These agents hold promise for improved diagnostic imaging and endoradiotherapy in oncology.