title: Radiolabeled peptide conjugates for targeting of the bombesin receptor superfamily subtypes.
abstract: Research laboratories around the world are currently focusing their efforts toward the development of radiometallated, site-directed, diagnostic/therapeutic agents based upon small peptides such as octreotide, neurotensin, alpha-melanocyte stimulating hormone, vasointestinal peptide and others. Bombesin (BBN) or derivatives of bombesin are also of significant interest. Bombesin is a 14-amino-acid peptide with very high affinity for the BB2 or gastrin-releasing peptide receptor (GRPr). Over-expression of the GRPr on a variety of human cancers (i.e., breast, prostate, pancreatic, small cell lung, etc.) provides potential efficacy toward development of radiometallated BBN derivatives for targeting and, hence, diagnosis/treatment of these specific diseases. New derivatives are being developed that are also capable of targeting the BB1 and BB3 receptor subtypes that are over-expressed on cancer cells. This review highlights some of the more recent developments toward design of BBN receptor-specific radiopharmaceuticals that have taken place over the past 2 years.
authors.affiliation: Research Services, H.S. Truman Memorial VA Hospital, Columbia, MO 65201, USA.
authors.forename: Charles J
authors.initials: CJ
authors.lastname: Smith
authors.forename: Wynn A
authors.initials: WA
authors.lastname: Volkert
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Hoffman
mesh_terms: D000818:Animals; D014408:Biomarkers, Tumor / Q000378:metabolism; D001839:Bombesin / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D016503:Drug Delivery Systems / Q000379:methods; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism / Q000532:radiotherapy; D010455:Peptides / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D011868:Radioisotopes / Q000737:chemistry / Q000378:metabolism* / Q000627:therapeutic use; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D018004:Receptors, Bombesin / Q000378:metabolism*
chemical_list: D014408:Biomarkers, Tumor; D010455:Peptides; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D018004:Receptors, Bombesin; D001839:Bombesin