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 overexpress/ 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.
Keywords: Bombesin, gastrin-releasing peptide, neuromedin B, BRS-3, receptor-mediated imaging, tumor cytotoxicity, DOTA, DTPA, NOTA, decapeptide, NMB, gastrinreleasing peptide receptor, GRPR, neuromedin B receptor, NMBR, G protein-coupled somatostatin receptors, myocardial perfusion imaging, functional brain imaging, immunoscintigraphy, tetraamine-benzyllaminidiglycolic acid, Litorin, ranatensin peptide family, Positron emission tomographic scanning, 1,4,7-triazacyclononanetriacetic acid, Radiolanthanides, Rhenium, BZH3, Camptothecin, topoisomerase I inhibitor, topoisomerase I, paclitaxel, Taxol, hemiasterlin, dolastatin, diphtheria toxin, Mitochondria-disrupting peptides, anti-FcRI, Mono-carbohexyl- tetrasulfonated aluminium phthalocyanine alone
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