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Prostate Cancer Theranostics Targeting Gastrin-Releasing Peptide Receptors
Lucia Baratto1, Hossein Jadvar2, Andrei Iagaru1
1Department of Radiology, Stanford University, Stanford, CA, USA.
Abstract:
Gastrin-releasing peptide receptors (GRPRs), part of the bombesin (BBN) family, are aberrantly overexpressed in many cancers, including those of the breast, prostate, pancreas, and lung, and therefore present an attractive target for cancer diagnosis and therapy. Different bombesin analogs have been radiolabeled and used for imaging diagnosis, staging, evaluation of biochemical recurrence, and assessment of metastatic disease in patients with prostate cancer. Recently, interest has shifted from BBN-like receptor agonists to antagonists, because the latter does not induce adverse effects and demonstrate superior in vivo pharmacokinetics. We review the preclinical and clinical literatures on the use of GRPRs as targets for imaging and therapy of prostate cancer, with a focus on the newer developments and theranostic potential of GRPR peptides.
Insights
Gastrin-releasing peptide receptors (GRPRs) are promising targets for diagnosing and treating cancers like prostate cancer. Newer GRPR antagonists offer improved safety and effectiveness for imaging and therapy.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Gastrin-releasing peptide receptors (GRPRs) are overexpressed in various cancers, including breast, prostate, pancreas, and lung.
- Bombesin (BBN) analogs targeting GRPRs have been utilized for prostate cancer imaging and staging.
- Recent research focuses on GRPR antagonists due to their improved safety and pharmacokinetics compared to agonists.
Purpose of the Study:
- To review preclinical and clinical literature on GRPR-targeted imaging and therapy for prostate cancer.
- To highlight recent advancements in GRPR-targeted agents.
- To discuss the theranostic potential of GRPR peptides.
Main Methods:
- Literature review of preclinical and clinical studies.
- Analysis of bombesin analogs, focusing on agonists and antagonists.
- Evaluation of imaging and therapeutic applications of GRPR-targeting agents.
Main Results:
- GRPRs are validated targets for prostate cancer diagnosis and therapy.
- Radiolabeled BBN analogs have shown utility in prostate cancer management.
- GRPR antagonists demonstrate advantages over agonists, including reduced adverse effects and better in vivo behavior.
Conclusions:
- GRPRs represent a significant target for developing novel prostate cancer diagnostics and therapeutics.
- The shift towards GRPR antagonists signifies a promising direction for theranostic applications.
- Further research into GRPR peptide theranostics holds potential for improved patient outcomes.
