ReviewChemistry & biodiversity2026
GRPR-Targeted Radionuclide Conjugates: A Molecular Evolution Perspective.
Review in Chemistry & biodiversity, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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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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Authors and funding
4 authors.
Funding
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Abstract
The gastrin-releasing peptide receptor (GRPR) serves as an important target for radiopharmaceutical conjugates in cancer diagnosis and therapy. This article systematically reviewed the evolution of GRPR-targeted ligands: from early agonists whose clinical application was limited by side effects, to current antagonists with improved stability and tumor retention. Key structural optimizations include C-terminal modifications of peptides, along with the design of linkers and chelators, which collectively enhance targeting capability and pharmacokinetic properties. Despite the significant progress achieved so far, challenges such as off-target uptake and inadequate metabolic stability still remain. Future research should be directed toward elucidating structure-activity relationships and designing novel ligands, linkers and chelators to promote the development of more selective and efficient diagnostic and therapeutic radiopharmaceuticals for cancers with high GRPR expression.
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