ReviewEJNMMI research2021
There is a world beyond αvβ3-integrin: Multimeric ligands for imaging of the integrin subtypes αvβ6, αvβ8, αvβ3, and α5β1 by positron emission tomography.
Review in EJNMMI research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 2 of them syntheses that pooled it.
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Who cites it
29 citing papers in PubMed, 2 syntheses or guidelines pooled it.
- Systematic Review: Targeted Molecular Imaging of Angiogenesis and Its Mediators in Rheumatoid Arthritis.International journal of molecular sciences · 2022Pooled it
- Overview of the RGD-Based PET Agents Use in Patients With Cardiovascular Diseases: A Systematic Review.Frontiers in medicine · 2022Pooled it
- Prospective Phase II Trial of [Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2023Trial
- Article
- Beyond conventional maging: the diagnostic performance of [Annals of nuclear medicine · 2026Article
- Linker Optimization in Lu-177 Labeled αvβ6-Integrin Binding Peptide Trimers for Targeted Radionuclide Therapy of Cancer.Molecular pharmaceutics · 2026Article
- Immunohistochemical Expression of Integrin αBiomolecules · 2026Article
- Tumour Microenvironment-Informed Radiotheranostics: Why and How Nuclear Medicine Could Advance Precision Oncology in the Decade Ahead.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Article
- Optimization of Methods for the Quantitative Analysis of Global Cell Surface Proteome and Cell Surface Polarization.International journal of molecular sciences · 2025Article
- The molecular blueprint of targeted radionuclide therapy.Nature reviews. Clinical oncology · 2025Review
- Integrin αvβ6-Targeted PET/CT Imaging of Non-Small Cell Lung Cancer with [Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Observational
- Antifibrotic Efficacy of a Nintedanib-Peptide Conjugate and Diagnostic Potential of a Fluorescent Companion Probe Targeting αACS pharmacology & translational science · 2025Article
- Review
- Switching Roles─Exploring Concentration-Dependent Agonistic versus Antagonistic Behavior of Integrin Ligands.Journal of medicinal chemistry · 2025Article
- Enhanced radiotheranostic targeting of integrinActa pharmaceutica Sinica. B · 2025Article
- Article
- Integrins and NAFLD-associated liver diseases: clinical associations, pathophysiological mechanisms and pharmacological implications.Acta biochimica et biophysica Sinica · 2024Review
- Lymphocytic Myocarditis in Children with Parvovirus B19 Infection: Pathological and Molecular Insights.Biomedicines · 2024Article
- The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics.RSC medicinal chemistry · 2024Article
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundIn the context of nuclear medicine and theranostics, integrin-related research and development was, for most of the time, focused predominantly on 'RGD peptides' and the subtype αvβ3-integrin. However, there are no less than 24 known integrins, and peptides without the RGD sequence as well as non-peptidic ligands play an equally important role as selective integrin ligands. On the other hand, multimerization is a well-established method to increase the avidity of binding structures, but multimeric radiopharmaceuticals have not made their way into clinics yet. In this review, we describe how these aspects have been interwoven in the framework of the German Research Foundation's multi-group interdisciplinary funding scheme CRC 824, yielding a series of potent PET imaging agents for selective imaging of various integrin subtypes.
resultsThe gallium-68 chelator TRAP was utilized to elaborate symmetrical trimers of various peptidic and non-peptidic integrin ligands. Preclinical data suggested a high potential of the resulting Ga-68-tracers for PET-imaging of the integrins α5β1, αvβ8, αvβ6, and αvβ3. For the first three, we provide some additional immunohistochemistry data in human cancers, which suggest several future clinical applications. Finally, application of αvβ3- and αvβ6-integrin tracers in pancreatic carcinoma patients revealed that unlike αvβ3-targeted PET, αvβ6-integrin PET is not characterized by off-target uptake and thus, enables a substantially improved imaging of this type of cancer.
conclusionsNovel radiopharmaceuticals targeting a number of different integrins, above all, αvβ6, have proven their clinical potential and will play an increasingly important role in future theranostics.
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