ArticleTheranostics2014
Dimerization of a phage-display selected peptide for imaging of αvβ6- integrin: two approaches to the multivalent effect.
Article in Theranostics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 35 citations in OpenAlex.
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- Monovalent and Divalent Designs of Copper Radiotheranostics Targeting Fibroblast Activation Protein in Cancer.Cancers · 2024Article
- A stapled chromogranin A-derived peptide homes in on tumors that express αvβ6 or αvβ8 integrins.International journal of biological sciences · 2023Article
- Versatile Synthesis of Multivalent Porphyrin-Peptide Conjugates by Direct Porphyrin Construction on Resin.Angewandte Chemie (International ed. in English) · 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
- Evaluation of Two Optical Probes for Imaging the Integrin αMolecular imaging and biology · 2020Article
- PET/CT Imaging of NSCLC with a αMolecular imaging and biology · 2019Article
- Therapeutic Radiopharmaceuticals Targeting Integrin αvβ6.ACS omega · 2018Article
- ImmunoPET Imaging of αMolecular imaging and biology · 2018Article
- Small-animal SPECT/CT imaging of cancer xenografts and pulmonary fibrosis using aBiophysics reports · 2018Article
- Multifunctional αBioconjugate chemistry · 2017Article
- Review
- Imaging the Tumor Microenvironment.Advances in experimental medicine and biology · 2017Review
- The Effect of Bi-Terminal PEGylation of an Integrin αvβ₆-Targeted ¹⁸F Peptide on Pharmacokinetics and Tumor Uptake.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2015Article
- Molecular imaging of integrin αvβ6 expression in living subjects.American journal of nuclear medicine and molecular imaging · 2014Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The integrin αvβ6 is an emerging biomarker for non-small cell lung cancer (NSCLC). An αvβ6-binding peptide was previously selected from a phage-displayed peptide library. Here, we utilize a multivalent design to develop a peptidic probe for positron emission tomography (PET) imaging of αvβ6+ NSCLC tumors. Multimeric presentation of this peptide, RGDLATLRQL, on a bifunctional copper chelator was achieved using two approaches: dimerization of the peptide followed by conjugation to the chelator (H2-D10) and direct presentation of two copies of the peptide on the chelator scaffold (H2-(M10)2). Binding affinities of the divalent peptide conjugates are four-fold higher than their monovalent counterpart (H2-M10), suggestive of multivalent binding. PET imaging using the bivalent 64Cu-labeled conjugates showed rapid and persistent accumulation in αvβ6+ tumors. By contrast, no significant accumulation was observed in αvβ6- tumors. Irrespective of the dimerization approach, all divalent probes showed three-fold higher tumor uptake than the monovalent probe, indicating the role of valency in signal enhancement. However, the divalent probes have elevated uptake in non-target organs, especially the kidneys. To abrogate nonspecific uptake, the peptide's N-terminus was acetylated. The resultant bivalent probe, 64Cu- AcD10, showed drastic decrease of kidney accumulation while maintaining tumor uptake. In conclusion, we developed an αvβ6-integrin specific probe with optimized biodistribution for noninvasive PET imaging of NSCLC. Further, we have demonstrated that use of multivalent scaffolds is a plausible method to improve library selected peptides, which would be suboptimal or useless otherwise, for imaging probe development.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.