A Novel Organometallic Aqua Complex of Technetium for the Labeling of Biomolecules:  Synthesis of [99mTc(OH2)3(CO)3]+ from [99mTcO4]- in Aqueous Solution and Its Reaction with a Bifunctional Ligand

Alberto, Roger; Schibli, Roger; Egli, André; Schubiger, August P.; Abram, Ulrich; Kaden, Thomas A.

doi:10.1021/ja980745t

Cited by 652 publications

(476 citation statements)

References 16 publications

(14 reference statements)

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“…[20][21][22] + moiety is consistent with a mixed ligand approach. [24] The reaction of [M(OH 2 ) 3 (CO) 3 1 H, 13 C, and 31 P NMR spectroscopic analysis confirmed the proposed composition (see Supporting Information).…”

supporting

confidence: 78%

Vitamin B12 as a Ligand for Technetium and Rhenium Complexes

et al. 2004

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supporting

confidence: 78%

Vitamin B12 as a Ligand for Technetium and Rhenium Complexes

et al. 2004

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“…A versatile route for labelling bombesin via the [ 99m Tc I -fac-(CO) 3 (H 2 O) 2 ] + -synthon [40] involved coupling of N α -histidinyl-acetic or 2-picolylamine-N,N-diacetic acid to BB (7)(8)(9)(10)(11)(12)(13)(14) [41,42] . But the resulting radiopeptides failed to accumulate effectively in PC-3 xenografts in nude mice (<0.6%ID/g at 1.5 h pi).…”

Section: Development and Preclinical Studies On Radiolabelled Bombesinsmentioning

confidence: 99%

Targeting prostate cancer with radiolabelled bombesins

Maina

Nock²,

Mather

2006

Cancer Imaging

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The fact that a number of common human tumours, including those of breast and prostate, express increased levels of the gastrin-releasing peptide receptor (GRP-R) means that this receptor is a potential target for peptide receptor mediated scintigraphy and targeted radionuclide therapy. Although clinical application is yet in its infancy, there is a considerable literature on preclinical studies aimed at developing suitable radioligands for potential clinical application. This brief review provides an overview of this research and also describes some of the limited clinical studies that have been published.

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“…Advances in the development of organometallic compounds and their cognate chelators for labeling biomolecules with 99m Tc has led to an outbreak of radiopharmaceutical molecules labeled with low oxidation state +1 99m Tc-Tricarbonyl [ 99m Tc(CO) 3 ] cores. The successful development of a kit preparation for the synthesis of the fac -[ 99m Tc (CO) 3 (OH 2 ) 3 ] + aquaion as a radiosynthon has led to the development of 99m Tc(CO) 3 -labeled antibodies, peptides, sugars and nucleotides [12,13]. Because of the low-spin, d 6 electronics configuration of Tc(I), the 99m Tc(CO) 3 core is remarkably stable over a wide range of pH values.…”

Section: Introductionmentioning

confidence: 99%

“…Because of the low-spin, d 6 electronics configuration of Tc(I), the 99m Tc(CO) 3 core is remarkably stable over a wide range of pH values. Alberto et al [12] first reported the one-step synthesis of Tc(I) complexes [ 99m Tc (OH 2 ) 3 (CO) 3 ] + by direct reduction of [ 99m Tc]pertechnetate with sodium borohydride in aqueous solution in the presence of carbon monoxide. In [ 99m Tc (OH 2 ) 3 (CO) 3 ] + all three water molecules are very labile with respect to substitution.…”

Section: Introductionmentioning

confidence: 99%

[99mTc(CO)3]-Radiolabeled Bevacizumab: In vitro and in vivo Evaluation in a Melanoma Model

Camacho

Garcia²,

Calzada³

et al. 2013

Oncology

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Introduction: Vascular endothelial growth factor (VEGF) is one of the classic factors to tumor-induced angiogenesis in several tumor types, including melanoma. Bevacizumab, a monoclonal antibody against VEGF, could be used as an imaging tool in preclinical studies. Objective: To radiolabel bevacizumab with [^99mTc(CO)₃(OH₂)₃]⁺ and evaluate it in vivo and in vitro for melanoma imaging properties. Methods: Bevacizumab was radiolabeled with [^99mTc(CO)₃(OH₂)₃]⁺ ion in saline. The radiochemical stability of the labeled antibody was assessed. The biodistribution and scintigraphy imaging of the radiolabeled antibody were evaluated in normal C57BL/6J mice and in C57BL/6J mice bearing murine B16F1 melanoma tumors. Immunoreactivity of bevacizumab to murine tumors was determined from direct immunofluorescence and immunoblotting assays. Results: We demonstrate that ^99mTc(CO)₃-bevacizumab was stable. In vivo biodistribution studies revealed that tumor uptake of ^99mTc(CO)₃-bevacizumab was 2.64 and 2.51 %ID/g at 4 and 24 h postinjection. Scintigraphy image studies showed tumor selective uptake of ^99mTc(CO)₃-bevacizumab in the tumor-bearing mice. This affinity was confirmed by immunoassays performed on B16F10 tumor samples. Conclusions:^99mTc(CO)₃-bevacizumab could be used as an approach for tumor nuclear imaging in preclinical studies. This should be useful to provide insights into the angiogenic stimulus before and after chemotherapy, which might help improve current antitumor therapy.

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A Novel Organometallic Aqua Complex of Technetium for the Labeling of Biomolecules: Synthesis of [^99mTc(OH₂)₃(CO)₃]⁺ from [^99mTcO₄]^- in Aqueous Solution and Its Reaction with a Bifunctional Ligand

Cited by 652 publications

References 16 publications

Vitamin B12 as a Ligand for Technetium and Rhenium Complexes

Vitamin B12 as a Ligand for Technetium and Rhenium Complexes

Targeting prostate cancer with radiolabelled bombesins

[<sup>99m</sup>Tc(CO)<sub>3</sub>]-Radiolabeled Bevacizumab: In vitro and in vivo Evaluation in a Melanoma Model

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