ArticleEJNMMI research2020
Tracking a TGF-β activator in vivo: sensitive PET imaging of αvβ8-integrin with the Ga-68-labeled cyclic RGD octapeptide trimer Ga-68-Triveoctin.
Article in EJNMMI research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 20 citations in OpenAlex.
- The molecular blueprint of targeted radionuclide therapy.Nature reviews. Clinical oncology · 2025Review
- Review
- Blockade of αvβ6 and αvβ8 integrins with a chromogranin A-derived peptide inhibits TGFβ activation in tumors and suppresses tumor growth.Journal of experimental & clinical cancer research : CR · 2025Article
- The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics.RSC medicinal chemistry · 2024Article
- Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction.RSC medicinal chemistry · 2023Article
- Click Chemistry and Radiochemistry: An Update.Bioconjugate chemistry · 2023Review
- RGD Forever!-Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences.Pharmaceuticals (Basel, Switzerland) · 2022Article
- PET/CT imaging of head-and-neck and pancreatic cancer in humans by targeting the "Cancer Integrin" αvβ6 with Ga-68-Trivehexin.European journal of nuclear medicine and molecular imaging · 2022Article
- It's Time to Shift the Paradigm: Translation and Clinical Application of Non-αvβ3 Integrin Targeting Radiopharmaceuticals.Cancers · 2021Review
- There is a world beyond αvβ3-integrin: Multimeric ligands for imaging of the integrin subtypes αvβ6, αvβ8, αvβ3, and α5β1 by positron emission tomography.EJNMMI research · 2021Review
- Recent Progress in the Molecular Imaging of Nonalcoholic Fatty Liver Disease.International journal of molecular sciences · 2021Review
- Review
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
purposeAs a major activator of transforming growth factor β (TGF-β), the RGD receptor αvβ8-integrin is involved in pathogenic processes related to TGF-β dysregulation, such as tumor growth, invasion, and radiochemoresistance, metastasis and tumor cell stemness, as well as epithelial-mesenchymal transition. The novel positron emission tomography (PET) radiopharmaceutical Ga-68-Triveoctin for in vivo mapping of αvβ8-integrin expression might enhance the prognosis of certain tumor entities, as well as support and augment TGF-β-targeted therapeutic approaches.
methodsMonomeric and trimeric conjugates of cyclo(GLRGDLp(NMe)K(pent-4-ynoic amide)) were synthesized by click chemistry (CuAAC), labeled with Ga-68, and evaluated in MeWo (human melanoma) xenografted SCID mice by means of PET and ex-vivo biodistribution. αvβ8-integrin expression in murine tissues was determined by β8-IHC. A human subject received a single injection of 173 MBq of Ga-68-Triveoctin and underwent 3 subsequent PET/CT scans at 25, 45, and 90 min p.i..
resultsThe trimer Ga-68-Triveoctin exhibits a 6.7-fold higher αvβ8-integrin affinity than the monomer (IC
conclusionGa-68-Triveoctin enables sensitive in-vivo imaging αvβ8-integrin expression in murine tumor xenografts. PET in a human subject confirmed a favorable biodistribution, underscoring the potential of Ga-68-Triveoctin for mapping of αvβ8-integrin expression in a clinical setting.
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