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A Novel d-Amino Acid-Composed GRPR-Targeted Peptide in Glioma
Xueyuan Ling1,2, Jiyun Shi3, Yutong Zhao4
1Department of Neurosurgery, Beijing Tiantan Hospital, National Center for Neurological Disorders, Capital Medical University, Beijing 100070, China.
Molecular Pharmaceutics
|January 7, 2026
Summary
This study developed a novel d-amino acid peptide, BBN(D), for improved glioma imaging. BBN(D)-based probes showed high specificity and tumor accumulation in preclinical models, offering potential for stable preoperative and intraoperative glioma detection.
Area of Science:
- Oncology
- Molecular Imaging
- Radiochemistry
Background:
- Gastrin-releasing peptide receptor (GRPR) is overexpressed in glioma.
- Existing Bombesin (BBN) imaging agents have limitations in in vivo stability.
- Novel d-amino acid-based BBN [BBN(D)] aims to overcome these limitations.
Purpose of the Study:
- To develop and evaluate a novel d-amino acid-composed peptide, BBN(D), for glioma imaging.
- To synthesize and test BBN(D)-based probes for near-infrared (NIR) fluorescence and PET/CT imaging.
- To assess the in vivo stability, specificity, and tumor accumulation of BBN(D) probes.
Main Methods:
- Synthesis of BBN(D)-Cy5.5 and [68Ga]Ga-DOTA-BBN(D) probes.
- Confirmation of probe identity and purity using HPLC and mass spectrometry.
- In vitro cell studies and in vivo imaging in subcutaneous and intracranial glioma xenograft models.
- Biodistribution studies and ex vivo tissue analysis.
Main Results:
- BBN(D)-based probes demonstrated high purity (>95%) and confirmed identity.
- In vitro studies showed specific binding of BBN(D)-Cy5.5 to GRPR-expressing cells.
- In vivo imaging revealed high specificity and tumor accumulation of both NIR fluorescence and PET/CT probes.
- Biodistribution confirmed enhanced tumor uptake and blood-brain barrier penetration of [68Ga]Ga-DOTA-BBN(D).
Conclusions:
- The d-amino acid-based BBN [BBN(D)] offers a stable and specific molecular imaging agent for glioma.
- BBN(D) probes show promise for both preoperative and intraoperative glioma detection.
- Further clinical exploration of BBN(D) for glioma imaging is warranted.
Keywords:
Cyanine5.5(Cy5.5)Gallium-68(68Ga)bombesind-amino acid peptidegastrin releasing peptide receptor(GRPR)near-infrared (NIR) fluorescencepositron emission tomography(PET)More Related Videos
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