ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2016
Tumor-Specific Binding of Radiolabeled PEGylated GIRLRG Peptide: A Novel Agent for Targeting Cancers.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 26 citations in OpenAlex.
- GRP78 dysregulation: A proposed molecular mechanism linking the tumor microenvironment to sepsis susceptibility in patients with cancer (Review).International journal of molecular medicine · 2026Review
- CAR immune cell therapy strategies and advances for lung cancer.Discover oncology · 2026Review
- Homoharringtonine exhibits senotherapeutic activity that mitigates diet- and age-associated obesity and insulin resistance and extends lifespan in mice.Nature communications · 2026Article
- Peptide Drugs in Gastrointestinal Tumors: Integrating Targeting, Delivery, and Therapeutic Actions for Synergistic Strategies.Biomolecules · 2026Review
- Enhancing Cytosolic Internalization of [International journal of molecular sciences · 2025Article
- Development of a [89Zr]Zr-labeled Human Antibody using a Novel Phage-displayed Human scFv Library.Clinical cancer research : an official journal of the American Association for Cancer Research · 2024Article
- Cell-Surface GRP78-Targeted Chimeric Antigen Receptor T Cells Eliminate Lung Cancer Tumor Xenografts.International journal of molecular sciences · 2024Article
- Blocking the functional domain of TIP1 by antibodies sensitizes cancer to radiation therapy.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2023Article
- Molecular imaging of HER2 expression in breast cancer patients using a novel peptide-based tracerJournal of translational medicine · 2023Article
- A human pan-cancer system analysis of heat shock protein family A member 5.American journal of cancer research · 2023Article
- Review
- GRP78 in lung cancer.Journal of translational medicine · 2021Review
- GRP78 targeting: Hitting two birds with a stone.Life sciences · 2020Review
- Noninvasive Classification of Human Triple Negative Breast Cancer by PET Imaging with GRP78-Targeted Molecular Probe [Molecular imaging and biology · 2020Article
- Development of Novel Radiosensitizers through the National Cancer Institute's Small Business Innovation Research Program.Radiation research · 2020Article
- PEGylated peptide to TIP1 is a novel targeting agent that binds specifically to various cancers in vivo.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- Immune targets in the tumor microenvironment treated by radiotherapy.Theranostics · 2019Review
- Impact of time-of-flight PET on quantification accuracy and lesion detection in simultaneousEJNMMI research · 2018Article
- New Insights in the Design of Bioactive Peptides and Chelating Agents for Imaging and Therapy in Oncology.Molecules (Basel, Switzerland) · 2017Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
Cancer-specific targeting sparing normal tissues would significantly enhance cancer therapy outcomes and reduce cancer-related mortality. One approach is to target receptors or molecules that are specifically expressed on cancer cells. Peptides as cancer-specific targeting agents offer advantages such as ease of synthesis, low antigenicity, and enhanced diffusion into tissues. Glucose-regulated protein 78 (GRP78) is an endoplasmic reticulum stress chaperone that regulates the unfolded protein response and is overexpressed in various cancers. In this study, we evaluated GIRLRG peptide that specifically targets GRP78 for cancer-specific binding (in vitro) and noninvasive tumor imaging (in vivo).
methodsGIRLRG peptide was modeled into the GRP78 ATPase domain using computational modeling. Surface plasmon resonance studies were performed to determine the affinity of GIRLRG peptide to GRP78 protein. GIRLRG was conjugated with PEG to prolong its circulation in mice. Tumor binding efficacy of PEG-GIRLRG peptide was evaluated in nude mice bearing heterotopic cervical (HT3), esophageal (OE33), pancreatic (BXPC3), lung (A549), and glioma (D54) tumors. Nano-SPECT/CT imaging of the mice was performed 48 and 72 h after injection with
resultsUsing molecular modeling and surface plasmon resonance, we identified that GIRLRG was binding with an affinity constant of 2.16 × 10
conclusionGIRLRG peptide specifically binds to the ATPase domain of GRP78. Radiolabeled PEG-GIRLRG could be used to target various cancers. Further studies would be required to translate PEG-GIRLRG peptide into the clinic.
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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.