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Study breakdown

Peptide Probe Targets NPY1R for Both Glioma Imaging and Alpha-Particle Therapy

RPEP-151852026Gan, Rong; Xu, Duling; Liu, Weihao; Liu, Jiadi; Yang, Yuanyou; Liu, Ning; Zhang, Qiyue; Wang, Zhimin; Li, Hongyan
evidence
The takeaway

A 68Ga/211At-labeled NPY1R-targeting peptide served as both a PET imaging agent and therapeutic radiopharmaceutical for glioma, demonstrating specific tumor uptake and treatment potential.

Image + treat

Same NPY1R-targeting peptide enables both diagnostic imaging (68Ga) and therapeutic radiation (211At) for brain tumors

What the researchers found

A 68Ga/211At-labeled NPY1R-targeting peptide demonstrated specific glioma uptake for PET imaging and therapeutic alpha-particle delivery, establishing a theranostic platform for brain tumors.

Why it matters

Gliomas have poor prognosis. A peptide that can both diagnose and treat brain tumors through the same receptor target could improve outcomes by enabling precise, personalized therapy.

How the study worked

Peptide synthesis and radiolabeling with 68Ga and 211At, binding affinity assays, biodistribution studies, PET imaging, and therapeutic efficacy assessment in glioma models.

What this study cannot tell us

Preclinical study. Alpha-particle therapy dosimetry in brain is complex. Blood-brain barrier penetration in humans needs confirmation.

How to read the evidence

Preclinical theranostic development with imaging and efficacy validation. Novel approach for glioma.

When this study was published

Published in 2025.

The bigger picture

Peptide-based theranostics combine diagnosis and therapy in one molecule. Success in glioma could establish this approach for other NPY1R-expressing tumors.

Questions still open

  • Can this peptide cross the blood-brain barrier sufficiently for clinical glioma treatment?
  • How does NPY1R expression vary across glioma grades?
  • Would combination with other treatments improve glioma outcomes?

Common questions

What is a theranostic?
A theranostic is a molecule that can both diagnose and treat disease. This peptide targets brain tumor cells and can carry either an imaging agent (for diagnosis) or a radioactive atom (for treatment).
How does this peptide find brain tumors?
Brain tumors overexpress NPY1R, a receptor for neuropeptide Y. The peptide specifically binds this receptor, concentrating at the tumor for imaging or delivering radiation directly to cancer cells.

Read the original research

68Ga/211At-Labeled Specific NPY1R Peptide-Based Molecular Probe for Glioma-Targeted Imaging and Alpha Therapy.

Biomacromolecules, 27(2), 1196-1209

View on PubMed ↗Publisher’s paper ↗

Citation

Gan, Rong; Xu, Duling; Liu, Weihao; Liu, Jiadi; Yang, Yuanyou; Liu, Ning; Zhang, Qiyue; Wang, Zhimin; Li, Hongyan. (2026). 68Ga/211At-Labeled Specific NPY1R Peptide-Based Molecular Probe for Glioma-Targeted Imaging and Alpha Therapy.. Biomacromolecules, 27(2), 1196-1209. https://doi.org/10.1021/acs.biomac.5c01407