Radiolabeled bombesin analogs for prostate cancer diagnosis: preclinical studies

Faintuch, Bluma Linkowski; Teodoro, Rodrigo; Duatti, Adriano; Muramoto, Emiko; Faintuch, Salomão; Smith, Charles J.

doi:10.1016/j.nucmedbio.2008.02.005

Cited by 71 publications

(52 citation statements)

References 24 publications

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“…Hydrolyzed wheat gluten (Sigma #H6784) was labeled with the radioactive nuclide technetium-99m ( 99m Tc), according to methods proposed by Faintuch et al (6) and de Barros et al (7). Evaluation of the radiolabeled yield was determined in vitro using thin layer chromatography, and stability of the radiolabeled complex 99m Tc-GLU in vivo was determined using scintigraphic images.…”

Section: Wheat Gluten Absorption and Biodistributionmentioning

confidence: 99%

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

et al. 2015

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Section: Wheat Gluten Absorption and Biodistributionmentioning

confidence: 99%

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

et al. 2015

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“…Tumor exhibited moderate uptake at 1 h post-administration; however, no reduction of tumor uptake was observed 4 h after injection, indicating the trapping of 99m Tc-BBN 7-14 in the tumor site due to the fact that GRP receptors are present on the surface of MDA-MB-231 cell line. 6 42 43 Tumor uptake for SpHLG-99m Tc-BBN 7-14 (1.2%ID/g) was twofold higher when compared with that of free 99m Tc-BBN 7-14 (0.6%ID/g, data not shown). These findings can be explained by the fact that these kinds of liposomes are themselves a targeting strategy for cancer therapy and/or diagnosis.…”

Section: Blood Clearancementioning

confidence: 88%

“…1 Cancer imaging techniques using radiotracers targeted to specific receptors have yielded successful results, demonstrating the utility of such approaches used to target these tumors, such as gastrin-releasing peptides, somatostatin, neurotensin, and vasoactive intestinal peptides. [5][6][7][8][9][10][11] Bombesin (BBN), a tetradecapeptide, was first isolated in 1971 from the skin of the European toad Bombina bombina. 12 The mammalian counterpart is the 27 amino acid gastrin-releasing peptide (GRP).…”

Section: Introductionmentioning

confidence: 99%

Bombesin Encapsulated in Long-Circulating pH-Sensitive Liposomes as a Radiotracer for Breast Tumor Identification

Barros¹,

Ld²,

Mm³

et al. 2015

j biomed nanotechnol

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Bombesin (BBN) is a tetradecapeptide that binds specifically to gastrin-releasing peptide receptors in humans. These receptors are over-expressed in several forms of cancer; radiolabeled BBN could therefore be used to detect such cancers. However, the degradation of peptides is a critical issue in the development of tumor tracers. Liposomes can be used to overcome this problem and improve the uptake of tracers by tumors. Therefore, the purpose of this study was to prepare and characterize long-circulating and pH-sensitive liposomes (SpHL) containing 99m Tc-HYNIC-Ala-Bombesin 7-14 ( 99m Tc-BBN 7-14 ). In addition, the ability of this system to identify human breast cancer tissue was evaluated using biodistribution studies and scintigraphic images. Long-circulating and pH-sensitive liposomes (SpHL) were prepared and freeze-dried in the presence of cryoprotectants (glucose, mannitol, and trehalose). They were subsequently reconstituted with a solution of 99m Tc-HYNIC-Ala-Bombesin 7-14 ( 99m Tc-BBN 7-14 ). The liposomes were evaluated for size, encapsulation percentage, radiotracer leakage, and storage stability. In addition, in vivo studies were performed in breast tumor-bearing nude mice. Liposomes in the presence of glucose (SpHLG), exhibited a mean diameter of 164.5 ± 6.5 nm and exhibited a 99m Tc-BBN 7-14 encapsulation percentage of 30%. In addition, they remained highly stable for up to 120 days of storage. SpHLG99m Tc-BBN 7-14 showed longer blood circulation than free 99m Tc-BBN 7-14 did. The tumor-to-muscle and tumor-to-blood ratios for SpHLG-99m Tc-BBN 7-14 were high at 4 h post-injection (9.31%ID/g and 7.93%ID/g, respectively). Furthermore, scintigraphic images revealed a strong signal in the tumor area, indicating tumor specificity of SpHLG-99m Tc-BBN 7-14 . In summary, SpHLG-99m Tc-BBN 7-14 presented characteristics suitable for a diagnostic agent, and is a potential tool for tumor identification.

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“…Co-injection of a big excess of native BN resulted in reduction in the uptake of radiolabeled peptides by intestines, tumor, and pancreas, confirming the presence of GRP-Rs in these organs. 76 In other organs such as liver and kidneys the concentration of radioactivity is increased after blocking experiments, possibly caused by the saturation effect of native BN in distribution and transport mechanisms.…”

Section: Discussionmentioning

confidence: 99%

Structural Assessment and Biological Evaluation of Two N₃S Bombesin Derivatives

et al. 2009

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The aim of the present study is the evaluation of the (99m)Tc complexes of two bombesin-like peptides: Gly1'-Gly2'-Cys3'-Aca-BN[2-14] (BN-1.1) and Gly1'-Gly2'-Cys3'-Aca-BN[7-14] (BN-1.1p). The BN derivatives were synthesized according to the solid phase peptide synthesis method, and characterized by ESI-MS and NMR. (185/187)Re-BN-1.1 and (185/187)Re-BN-1.1p were also identified by ESI-MS and NMR. The (99m)Tc complexes were stable over time in human plasma, while they degraded rapidly in kidney-liver homogenates. The peptides and their (99m)Tc complexes showed high affinity for the human GRP receptors expressed in PC-3 cells. The rate of internalization of these radiolabeled biomolecules was found to be time-dependent. Also, it was found that there was no long-term retention of the radioactive metabolites into the cells. Tissue distribution of the radiopeptides was evaluated in normal mice and in prostate cancer experimental models. Significant uptake of radioactivity was observed in the pancreas of PC-3 tumor-bearing SCID mice. Dynamic studies of both radiopeptides showed satisfactory tumor images.

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Radiolabeled bombesin analogs for prostate cancer diagnosis: preclinical studies

Cited by 71 publications

References 24 publications

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

Bombesin Encapsulated in Long-Circulating pH-Sensitive Liposomes as a Radiotracer for Breast Tumor Identification

Structural Assessment and Biological Evaluation of Two N₃S Bombesin Derivatives

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Radiolabeled bombesin analogs for prostate cancer diagnosis: preclinical studies

Cited by 71 publications

References 24 publications

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

Wheat gluten intake increases weight gain and adiposity associated with reduced thermogenesis and energy expenditure in an animal model of obesity

Bombesin Encapsulated in Long-Circulating pH-Sensitive Liposomes as a Radiotracer for Breast Tumor Identification

Structural Assessment and Biological Evaluation of Two N3S Bombesin Derivatives

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Structural Assessment and Biological Evaluation of Two N₃S Bombesin Derivatives