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Updated: May 8, 2026
Gene Regulation and Targeted Therapy in Gastric Cancer Peritoneal Metastasis: Radiological Findings from Dual Energy CT and PET/CT
Published on: January 22, 2018
Targeted radiotherapy with tumor vascular homing trimeric GEBP11 peptide evaluated by multimodality imaging for
Jing Zhang1, Hao Hu1, Shuhui Liang1
1State Key Laboratory of Cancer Biology & Xijing Hospital of Digestive Diseases, Fourth Military Medical University, Xi'an, China.
Abstract:
Targeted radiopharmaceutical is an effective treatment for solid tumors. By labeling with radionuclides, targeting peptide could achieve both noninvasive diagnosis and targeted radionuclide therapy. In order to evaluate the potential applicability of GEBP11 peptides in diagnosis and radiotherapy of gastric cancer, in this study, iodine 131 labeled GEBP11 peptides, including a novel bifid PEGlylated GEBP11 trimer and its corresponding monomer, were developed. The clinical potential of GEBP11 peptides, such as tumor binding affinity and antitumor efficacy was demonstrated and assessed with multimodality imaging methods. Cerenkov and SPECT imaging showed higher tumor uptake for (131)I-2PEG-(GEBP11)3 (P<0.05, day 1; P<0.01, day 2; vs. monomer). Biodistribution studies indicated higher tumor accumulation and better T/NT of (131)I-2PEG-(GEBP11)3. Bioluminescence imaging exhibited a significant tumor growth suppression in (131)I-2PEG-(GEBP11)3 treated group (P<0.001 vs. control; P<0.01 vs. monomer). After treatment with (131)I-2PEG-(GEBP11)3, the tumor volume and vasculature decreased significantly, and the survival time was prolonged to 75.5days. Meanwhile, no significant hepatic or renal toxicity was observed with (131)I-2PEG-(GEBP11)3 administered. In conclusion, (131)I-2PEG-(GEBP11)3 could be a promising candidate for peptide-based targeting therapy of gastric cancer. 2PEG-(GEBP11)3 might be a potential drug delivery vehicle for the antiangiogenic therapy of gastric cancer.
Insights
A novel iodine 131 labeled peptide, (131)I-2PEG-(GEBP11)3, shows promise for gastric cancer diagnosis and therapy. This targeted radiopharmaceutical effectively suppresses tumor growth and prolongs survival with minimal toxicity.
Area of Science:
- Oncology
- Radiopharmaceutical Therapy
- Molecular Imaging
Background:
- Targeted radiopharmaceuticals offer effective treatment for solid tumors.
- Peptide-based agents enable noninvasive diagnosis and targeted radionuclide therapy.
- Gastric cancer requires novel therapeutic strategies for improved outcomes.
Purpose of the Study:
- To evaluate the diagnostic and therapeutic potential of iodine 131 labeled GEBP11 peptides for gastric cancer.
- To develop and assess a novel bifid polyethylene glycol (PEGylated) GEBP11 trimer and its monomer.
- To investigate tumor binding affinity and antitumor efficacy using multimodality imaging.
Main Methods:
- Development of iodine 131 labeled GEBP11 peptides, including a novel bifid PEGylated trimer (2PEG-(GEBP11)3) and its monomer.
- Assessment of tumor uptake using Cerenkov and SPECT imaging.
- Evaluation of biodistribution, tumor-to-nontumor ratios (T/NT), and antitumor efficacy via bioluminescence imaging.
- Analysis of tumor volume, vasculature, and survival rates post-treatment.
- Monitoring for hepatic and renal toxicity.
Main Results:
- (131)I-2PEG-(GEBP11)3 demonstrated significantly higher tumor uptake compared to the monomer in Cerenkov and SPECT imaging.
- Biodistribution studies confirmed greater tumor accumulation and improved T/NT ratios for (131)I-2PEG-(GEBP11)3.
- Bioluminescence imaging revealed significant tumor growth suppression and prolonged survival (75.5 days) in the (131)I-2PEG-(GEBP11)3 treated group.
- Significant reduction in tumor volume and vasculature was observed.
- No significant hepatic or renal toxicity was detected.
Conclusions:
- (131)I-2PEG-(GEBP11)3 is a promising candidate for peptide-based targeted therapy of gastric cancer.
- The novel bifid PEGylated GEBP11 trimer shows potential as a drug delivery vehicle for antiangiogenic therapy in gastric cancer.
- This approach offers a dual modality for diagnosis and therapy with favorable safety profile.
