ArticleJournal of controlled release : official journal of the Controlled Release Society2016
Activatable iRGD-based peptide monolith: Targeting, internalization, and fluorescence activation for precise tumor imaging.
Article in Journal of controlled release : official journal of the Controlled Release Society, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 44 citations in OpenAlex.
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- Genetically programmable protein-biomineral core-shell nanovectors for enhancing tumor microenvironment-activated chemotherapy.Materials today. Bio · 2026Article
- Green/red fluorescent protein disrupting drugs for real-time permeability tracking in three-dimensional tumor spheroids.Bioengineering & translational medicine · 2025Article
- Enhanced tumor targeting and penetration of fluorophores via iRGD peptide conjugation: a strategy for the precision targeting of lung cancer.Translational lung cancer research · 2024Article
- Quenched Zwitterionic Cyclic Arg-Gly-Asp-Containing Pentapeptide Probe for Real-Time Brain Tumor Imaging.Pharmaceutics · 2024Article
- Intracavitary Applications for CEUS in PTCD.Diagnostics (Basel, Switzerland) · 2024Review
- Tumor-Homing Peptides as Crucial Component of Magnetic-Based Delivery Systems: Recent Developments and Pharmacoeconomical Perspective.International journal of molecular sciences · 2024Review
- Construction of Targeting-Peptide-Based Imaging Reagents and Their Application in Bioimaging.Chemical & biomedical imaging · 2024Review
- A Targeted Multi-Crystalline Manganese Oxide as a Tumor-Selective Nano-Sized MRI Contrast Agent for Early and Accurate Diagnosis of Tumors.International journal of nanomedicine · 2024Article
- RGD peptide in cancer targeting: Benefits, challenges, solutions, and possible integrin-RGD interactions.Cancer medicine · 2024Review
- Generation of peptides using phage display technology for cancer diagnosis and molecular imaging.Molecular biology reports · 2023Review
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- Ginsenosides emerging as both bifunctional drugs and nanocarriers for enhanced antitumor therapies.Journal of nanobiotechnology · 2021Review
- Hybrid Nanosystems for Biomedical Applications.ACS nano · 2021Review
- GSH-responsive SN38 dimer-loaded shape-transformable nanoparticles with iRGD for enhancing chemo-photodynamic therapy.Acta pharmaceutica Sinica. B · 2020Article
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- Peptide-Drug Conjugates and Their Targets in Advanced Cancer Therapies.Frontiers in chemistry · 2020Review
- RGD conjugated cell uptake off to on responsive NIR-AZA fluorophores: applications toward intraoperative fluorescence guided surgery.Chemical science · 2019Article
- iRGD: A Promising Peptide for Cancer Imaging and a Potential Therapeutic Agent for Various Cancers.Journal of oncology · 2019Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
Abstract
A disulfide-bridged cyclic RGD peptide, named iRGD (internalizing RGD, c(CRGDK/RGPD/EC)), is known to facilitate tumor targeting as well as tissue penetration. After the RGD motif-induced targeting on αv integrins expressed near tumor tissue, iRGD encounters proteolytic cleavage to expose the CendR motif that promotes penetration into cancer cells via the interaction with neuropilin-1. Based on these proteolytic cleavage and internalization mechanism, we designed an iRGD-based monolithic imaging probe that integrates multiple functions (cancer-specific targeting, internalization and fluorescence activation) within a small peptide framework. To provide the capability of activatable fluorescence signaling, we conjugated a fluorescent dye to the N-terminal of iRGD, which was linked to the internalizing sequence (CendR motif), and a quencher to the opposite C-terminal. It turned out that fluorescence activation of the dye/quencher-conjugated monolithic peptide probe requires dual (reductive and proteolytic) cleavages on both disulfide and amide bond of iRGD peptide. Furthermore, the cleavage of the iRGD peptide leading to fluorescence recovery was indeed operative depending on the tumor-related angiogenic receptors (αvβ3 integrin and neuropilin-1) in vitro as well as in vivo. Compared to an 'always fluorescent' iRGD control probe without quencher conjugation, the dye/quencher-conjugated activatable monolithic peptide probe visualized tumor regions more precisely with lower background noise after intravenous injection, owing to the multifunctional responses specific to tumor microenvironment. All these results, along with minimal in vitro and in vivo toxicity profiles, suggest potential of the iRGD-based activatable monolithic peptide probe as a promising imaging agent for precise tumor diagnosis.
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Registered trials
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.