Biodistribution and dosimetry of 99mTc RP527, a gastrin releasing peptide agonist for the visualisation of GRP-receptor expressing malignancies

Wiele, Christophe Van de; Dumont, Filip; Dierckx, Rudi; Peers, Susan H.; Thornback, John R.; Slegers, Guido; Thierens, Hubert

doi:10.1097/00006231-200006000-00078

Cited by 56 publications

(84 citation statements)

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“…However, similar strategies have been used for years in the field of positron emission tomography (PET), which often involves incorporation of a radioactive nucleus into a ligand of interest shortly before administration to a patient. For example, biological peptides of interest bearing artificial amino acid side-chains as chelating groups can be ''tagged'' with positron-emitting isotopes such as technecium-99 and delivered to a patient (23,24). These labeled tracers can then be assessed in vivo, using a gamma camera.…”

Section: Discussionmentioning

confidence: 99%

Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride

Wilson

Hurd²,

Keshari

et al. 2009

Proc. Natl. Acad. Sci. U.S.A.

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In this manuscript, the remarkable NMR signal enhancement that can be provided by dynamic nuclear polarization (DNP) was combined with the reactivity of acetic anhydride with amines to perform rapid, high SNR analyses of amino acid mixtures and to hyperpolarize new biomolecules of interest. [1,1-13 C] acetic anhydride is an excellent substrate for DNP hyperpolarization because it can be well polarized in only 30 min and has a relatively long T1 relaxation time (33.9 s at 11.7 T and 37°C). The secondary hyperpolarization approach developed in this project takes advantage of the preferential reaction of acetic anhydride with amine nucleophiles, which occurs much more rapidly than hydrolysis to produce hyperpolarized N-acetyl adducts. This new approach was used to reproducibly and near-quantitatively (mean yield ؊ 89.8%) resolve a mixture of amino acids Gly, Ser, Val, Leu, and Ala in a single acquisition (3 s) with a signal enhancement of up to 1,400-fold as compared with thermal equilibrium. Secondary hyperpolarization was performed for several small peptides and N-acetylcysteine, a drug administered intravenously to treat acetaminophen overdose. Although, in general the T1 of the N-acetyl adducts decreased with increasing molecular weight of the biomolecules, the T1 values were still on the order of 10 s, and the correlation of T1 with molecular weight was not exact suggesting the potential of secondarily polarizing relatively large biomolecules. This study demonstrates the feasibility of using prepolarized [1,1-13 C] acetic anhydride and rapid chemical reactions to provide high SNR NMR spectra of amino acid derivatives and other biomolecules.acetylation ͉ metabolism ͉ peptides ͉ spectroscopy

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Section: Discussionmentioning

confidence: 99%

Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride

Wilson

Hurd²,

Keshari

et al. 2009

Proc. Natl. Acad. Sci. U.S.A.

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“…For example, 99m Tcand 111 In-coupled BN analogues have been developed for diagnostic SPECT imaging and 64 Cu-and 68 Ga-labelled analogues for PET imaging of GRP receptor-expressing tumours [26][27][28][29][30][31][32][33][34][35][36][37][38][39]. In addition, 90 Y-and 177 Lu-labelled analogues have been described as promising tools for targeted radiotherapy of these tumours [26,40].…”

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confidence: 99%

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Visser

Bernard

Erion

et al. 2007

Eur J Nucl Med Mol Imaging

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Purpose It has been shown that some primary human tumours and their metastases, including prostate and breast tumours, overexpress gastrin-releasing peptide (GRP) (5-14)), was tested in vivo in biodistribution studies using rats bearing GRP receptor-expressing CA20948 tumours, and nude mice bearing human PC3 xenografts. Injection of 111In-labelled Cmp 3 in these animals showed high, receptor-mediated uptake in receptor-positive organs and tumours which could be visualised using planar gamma camera and microSPECT/CT imaging. Conclusion With their enhanced receptor affinity and their rapid receptor-mediated internalisation in vitro and in vivo, the new BN analogues, and especially Cmp 3, are promising candidates for use in diagnostic molecular imaging and targeted radionuclide therapy of GRP receptor-expressing cancers.

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“…In fact, there have been various radiolabeled bombesin conjugates containing extensive modifications to the N-terminus, which still retain high affinity for the desired receptors (Baidoo et al 1998;La Bella et al 2002;Smith et al 2003; Van de Wiele et al 2001). Consequently, most labeled bombesin analogs are simply modifications of this bombesin-(7-14) sequence (Baidoo et al 1998;La Bella et al 2002;Smith et al 2003; Van de Wiele et al 2001; Van de Wiele et al 2000). In this case, modification of the bombesin-(7-14) peptide was carried out to include a second β-alanine extension in position six, replacing the non-essential D-Tyr (Fig.…”

Section: Peptide Synthesismentioning

confidence: 99%

Synthesis of bombesin-functionalized iron oxide nanoparticles and their specific uptake in prostate cancer cells

et al. 2009

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The imaging of molecular markers associated with disease offers the possibility for earlier detection and improved treatment monitoring. Receptors for gastrin-releasing peptide are overexpressed on prostate cancer cells offering a promising imaging target, and analogs of bombesin, an amphibian tetradecapeptide have been previously demonstrated to target these receptors. Therefore, the pan-bombesin analog [β-Ala11, Phe13, Nle14]bombesin-(7-14) was conjugated through a linker to dye-functionalized superparamagnetic iron oxide nanoparticles for the development of a new potential magnetic resonance imaging probe. The peptide was conjugated via click chemistry, demonstrating a complementary alternative methodology to CIHR Author ManuscriptCIHR Author Manuscript CIHR Author Manuscript conventional peptide-nanoparticle conjugation strategies. The peptide-functionalized nanoparticles were then demonstrated to be selectively taken up by PC-3 prostate cancer cells relative to unfunctionalized nanoparticles and this uptake was inhibited by the presence of free peptide, confirming the specificity of the interaction. This study suggests that these nanoparticles have the potential to serve as magnetic resonance imaging probes for the detection of prostate cancer.

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Biodistribution and dosimetry of 99mTc RP527, a gastrin releasing peptide agonist for the visualisation of GRP-receptor expressing malignancies

Cited by 56 publications

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Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride

Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Synthesis of bombesin-functionalized iron oxide nanoparticles and their specific uptake in prostate cancer cells

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Biodistribution and dosimetry of 99mTc RP527, a gastrin releasing peptide agonist for the visualisation of GRP-receptor expressing malignancies

Cited by 56 publications

References 0 publications

Generation of hyperpolarized substrates by secondary labeling with [1,1- 13 C] acetic anhydride

Generation of hyperpolarized substrates by secondary labeling with [1,1- 13 C] acetic anhydride

Novel 111In-labelled bombesin analogues for molecular imaging of prostate tumours

Synthesis of bombesin-functionalized iron oxide nanoparticles and their specific uptake in prostate cancer cells

Contact Info

Product

Resources

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Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride

Generation of hyperpolarized substrates by secondary labeling with [1,1- ¹³ C] acetic anhydride