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Published on: February 17, 2022
Bombesin receptor-mediated imaging and cytotoxicity: review and current status
Veronica Sancho1, Alessia Di Florio, Terry W Moody
1Digestive Diseases Branch, National Institutes of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
Abstract:
The three mammalian bombesin (Bn) receptors (gastrin-releasing peptide [GRP] receptor, neuromedin B [NMB] receptor, BRS-3) are one of the classes of G protein-coupled receptors that are most frequently over-express/ectopically expressed by common, important malignancies. Because of the clinical success of somatostatin receptor-mediated imaging and cytotoxicity with neuroendocrine tumors, there is now increasing interest in pursuing a similar approach with Bn receptors. In the last few years then have been more than 200 studies in this area. In the present paper, the in vitro and in vivo results, as well as results of human studies from many of these studies are reviewed and the current state of Bn receptor-mediated imaging or cytotoxicity is discussed. Both Bn receptor-mediated imaging studies as well as Bn receptor-mediated tumoral cytotoxic studies using radioactive and non-radioactive Bn-based ligands are covered.
Insights
Mammalian bombesin (Bn) receptors are frequently overexpressed in cancers. This review covers current research on Bn receptor-mediated imaging and cytotoxicity for cancer therapy, building on somatostatin receptor success.
Area of Science:
- Oncology
- Molecular Biology
- Radiopharmaceuticals
Background:
- Mammalian bombesin (Bn) receptors, including gastrin-releasing peptide (GRP) receptor, neuromedin B (NMB) receptor, and BRS-3, are G protein-coupled receptors.
- These receptors are frequently overexpressed or ectopically expressed in common and significant malignancies.
- Clinical success of somatostatin receptor-targeted therapies for neuroendocrine tumors has spurred interest in similar strategies for Bn receptors.
Purpose of the Study:
- To review the current state of bombesin (Bn) receptor-mediated imaging and cytotoxicity in cancer.
- To consolidate in vitro, in vivo, and human study results from over 200 recent investigations.
- To discuss the potential of Bn receptor-targeted approaches for cancer diagnosis and treatment.
Main Methods:
- Review of existing literature on Bn receptor-mediated imaging and cytotoxicity.
- Analysis of in vitro and in vivo experimental data.
- Evaluation of human clinical study findings.
Main Results:
- Significant research interest and over 200 studies in the past few years focusing on Bn receptors.
- Bn receptor-mediated imaging and cytotoxic studies utilize both radioactive and non-radioactive Bn-based ligands.
- Data from various studies indicate potential for Bn receptor-targeted diagnostics and therapeutics.
Conclusions:
- Bombesin (Bn) receptors represent a promising target for cancer imaging and therapy.
- Further development of Bn receptor-based ligands is crucial for clinical translation.
- Bn receptor-targeted strategies hold potential for improving cancer patient outcomes.
