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Bombesin Receptor-Mediated Imaging and Cytotoxicity: Review and Current Status

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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.





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

Document Type: Research Article

Publication date: January 1, 2011

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  • The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves.

    The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.

    The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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