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Published on: January 7, 2019
GRPR-Targeted Radionuclide Conjugates: A Molecular Evolution Perspective
Meng Li1,2,3, Yu Liu4, MengChao Cui3
1HTA Co., Ltd, Beijing, China.
Chemistry & Biodiversity
|July 28, 2026
Summary
Gastrin-releasing peptide receptor (GRPR) targeted radiopharmaceuticals are advancing for cancer care. Ligand design improvements enhance tumor targeting, but challenges in stability and specificity remain for future development.
Area of Science:
- Oncology
- Radiopharmaceutical Science
- Medicinal Chemistry
Background:
- The gastrin-releasing peptide receptor (GRPR) is a key target for developing targeted radiopharmaceuticals for cancer diagnosis and therapy.
- Early GRPR-targeted agonists faced limitations due to side effects and poor clinical applicability.
Purpose of the Study:
- To systematically review the evolution of GRPR-targeted ligands.
- To highlight structural optimizations and their impact on targeting capability and pharmacokinetics.
- To identify remaining challenges and future research directions in GRPR-targeted radiopharmaceuticals.
Main Methods:
- Systematic literature review focusing on the development of GRPR-targeted ligands.
- Analysis of structural modifications in peptide-based ligands, including C-terminal changes.
- Evaluation of linker and chelator designs for enhancing radiopharmaceutical properties.
Main Results:
- GRPR antagonists show improved stability and tumor retention compared to earlier agonists.
- Structural optimizations, including C-terminal modifications and advanced linker/chelator designs, enhance targeting and pharmacokinetics.
- Despite progress, challenges persist regarding off-target uptake and metabolic stability of current ligands.
Conclusions:
- Significant advancements have been made in GRPR-targeted ligand design for cancer radiopharmaceuticals.
- Further research is needed to overcome limitations such as off-target uptake and metabolic instability.
- Future efforts should focus on structure-activity relationships and novel designs for more selective and effective diagnostic and therapeutic agents for GRPR-expressing cancers.
