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

Area of Science:

• Oncology
• Radiochemistry
• Molecular Imaging

Background:

• Neuropeptide Y receptor Y1 (NPY1R) is a potential target for glioma treatment.
• Development of targeted radiopharmaceuticals is crucial for effective glioma imaging and therapy.

Purpose of the Study:

• To design and synthesize novel ⁶⁸Ga/²¹¹At-labeled NPY1R-targeting peptides for glioma.
• To evaluate the efficacy of these radiopharmaceuticals in preclinical glioma models.

Main Methods:

• Peptide sequences were designed using Molecular Operating Environment (MOE).
• The peptide KINW was synthesized and radiolabeled with ⁶⁸Ga and ²¹¹At.
• In vitro and in vivo studies were conducted using U87-MG cell lines and xenograft models.

Main Results:

• ⁶⁸Ga-labeled KINW showed enhanced uptake in glioma xenografts, indicating potential for imaging.
• ²¹¹At-labeled KINW (²¹¹At-ATE-KINW) demonstrated improved stability and efficacy, suppressing tumor growth and prolonging survival.
• ²¹¹At-ATE-KINW exhibited minimal retention in normal tissues.

Conclusions:

• A novel NPY1R-targeting peptide (KINW) was successfully developed.
• ⁶⁸Ga/²¹¹At-labeled KINW shows significant potential as a theranostic radiopharmaceutical for glioma.
• This peptide offers a promising avenue for targeted glioma imaging and therapy.