Bombesin analogues for gastrin-releasing peptide receptor imaging

Nanda, Prasant Kumar; Pandey, Usha; Bottenus, Brienne N.; Rold, Tammy L.; Sieckman, Gary L.; Szczodroski, Ashley F.; Hoffman, Timothy J.; Smith, Charles J.

doi:10.1016/j.nucmedbio.2011.10.009

Cited by 32 publications

(32 citation statements)

References 26 publications

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“…Micro-PET/CT imaging showed clear visualization of tumors 15 hours postinjection, whereas the more hydrophilic peptide had the highest accumulation in GRPR-expressing tumor and the most efficient clearance of radiotracer from whole body via the renal urinary excretion pathway ( Fig. 10) (Nanda et al, 2012).…”

Section: A Sustaining Proliferative Signalingmentioning

confidence: 99%

“…This is based on the idea that it might detect neuroendocrine differentiation, characteristic of high grade and high stage tumors, and might improve lymph node staging and recurrence detection (Koopmans et al, 2009;Abiraj et al, 2011;Lears et al, 2011). Nanda et al (2012) recently reported on the design, development, 64 Cu labeling, and evaluation of new bombesin antagonist analogs, 64 Cu-(NO2A-X-D-Phe 6 -BBN(6-13)NHEt. These peptides have different linker groups that determine the hydrophobicity that reflects on their pharmacokinetics in vivo.…”

Section: A Sustaining Proliferative Signalingmentioning

confidence: 99%

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Interrogating Tumor Metabolism and Tumor Microenvironments Using Molecular Positron Emission Tomography Imaging. Theranostic Approaches to Improve Therapeutics

Jacobson¹,

Chen²

2013

Pharmacol Rev

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Section: A Sustaining Proliferative Signalingmentioning

confidence: 99%

Section: A Sustaining Proliferative Signalingmentioning

confidence: 99%

Interrogating Tumor Metabolism and Tumor Microenvironments Using Molecular Positron Emission Tomography Imaging. Theranostic Approaches to Improve Therapeutics

Jacobson¹,

Chen²

2013

Pharmacol Rev

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“…After successful preclinical studies revealing a high binding affinity, good in vivo stability, and excellent targeting efficacy in PC-3 xenografts, this radiotracer exhibited encouraging results in the first clinical study. The same peptide was modified by adding hydrophobic spacers of different lengths (aminohexanoic acid [Ahx [6][7][8][9] ]) and functionalized with NOTA for 64 Cu complexation (24).…”

Section: Grpr Antagonistsmentioning

confidence: 99%

Bombesin-Targeted PET of Prostate Cancer

et al. 2016

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“…Gastrin-releasing peptide receptor (GRPR) primarily overexpressed in androgen-independent human prostate tissues (11) provides another potential target for prostate cancer diagnosis and therapy. Bombesin is an analog of gastrin-releasing peptide and the truncated sequence bombesin(7-14) (BBN) is considered to be capable of the specific binding to GRPR and metabolically stable for in vivo application (12,13). During the processes of angiogenesis, invasion, and metastasis of the GRPRpositive tumors, the activated endothelial cells around the tumor tissues can express a high level of integrin a v b 3 .…”

mentioning

confidence: 99%

In Vivo Cancer Dual-Targeting and Dual-Modality Imaging with Functionalized Quantum Dots

Wang

Tang

et al. 2015

J Nucl Med

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Semiconductor quantum dots (QDs), after surface modification to provide water solubility and biocompatibility, have a promising future in biomedical applications. In this study, a dual receptortargeting dual-modality PET/near-infrared fluorescence (NIRF) probe was developed for accurate assessment of the pharmacokinetics and tumor-targeting efficacy of QDs. Methods: QDs were modified by b-Glu-RGD-BBN (RGD is arginine-glycine-aspartate acid, and BBN is bombesin) peptides and then labeled with 18 F via the 4-nitrophenyl-2-18 F-fluoropropionate prosthetic group. Cytotoxicity and cell-binding assay of QD-RGD-BBN were performed with PC-3 cells. In vivo dual-modality PET/NIRF imaging of prostate tumor-bearing mice was investigated using QD-RGD-BBN and 2-18 F-fluoropropionyl-QD-RGD-BBN ( 18 F-FP-QD-RGD-BBN). An in vivo biodistribution study of 18 F-FP-QD-RGD-BBN was performed on normal mice. Results: QD-RGD-BBN exhibited strong red luminescence (600-800 nm) with the same maximum fluorescence wavelength (705 nm) as QD705 and slightly lower toxicity than that of QD705 in PC-3 cells at concentrations of greater than 30 mg/mL. Uptake of QD-RGD-BBN in PC-3 cells showed no significant decrease in the presence of an excess amount of dimer arginineglycine-aspartate acid (RGD 2 ) or bombesin(7-14) (BBN) peptide but was blocked significantly in the presence of an excess amount of NH 2 -RGD-BBN. Dual-function PET/NIRF imaging is able to accurately assess the biodistribution and tumor-targeting efficacy of the 18 F-labeled functionalized QDs. Conclusion: The functionalized QD probe has great potential as a universal dual-targeting probe for detecting tumors in living subjects, opening up a new strategy for the development of multitargeting multimodality 18 F-labeled QD probes with improved tumor-targeting efficacy.

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Bombesin analogues for gastrin-releasing peptide receptor imaging

Cited by 32 publications

References 26 publications

Interrogating Tumor Metabolism and Tumor Microenvironments Using Molecular Positron Emission Tomography Imaging. Theranostic Approaches to Improve Therapeutics

Interrogating Tumor Metabolism and Tumor Microenvironments Using Molecular Positron Emission Tomography Imaging. Theranostic Approaches to Improve Therapeutics

Bombesin-Targeted PET of Prostate Cancer

In Vivo Cancer Dual-Targeting and Dual-Modality Imaging with Functionalized Quantum Dots

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