Assessment of the best N3− donors in preparation of [M(N)(PNP)]-based (M=99mTc-; 188Re) target-specific radiopharmaceuticals: Comparison among succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG600-DTCZ)

Carta, Davide; Jentschel, Christian; Thieme, Stefan Felix; Salvarese, Nicola; Morellato, N.; Refosco, Fiorenzo; Ruzza, Paolo; Bergmann, Ralf; Pietzsch, Hans‐Jürgen; Bolzati, Cristina

doi:10.1016/j.nucmedbio.2014.04.126

Cited by 11 publications

(13 citation statements)

References 24 publications

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“…Elution was performed at 1.0 ml/min flow rate with a binary gradient system of 0.1% trifluoroacetic acid in acetonitrile as mobile phase (A) and 0.1% trifluoroacetic acid in water as mobile phase (B). The elution profile was as follows: 0 to 3 min, 100% A; 3 to 10 min, linear gradient to 100% B; and 10–20 min 100% B (Carta et al, ).…”

Section: Methodsmentioning

confidence: 99%

Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

et al. 2019

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The aim of this work was to develop and evaluate a 99m Tc-labeled neuropeptide Y derivative with affinity toward Y1-receptor. The selected amino acid sequence included nine amino acids derived from the C-terminal portion of the NPY complemented with the addition of one cysteine-mercaptoacetic acid moiety to bind the radiometal. Labeling was achieved through the preparation of a 3 + 1 nitrido complex. Physicochemical evaluation, cell uptake, internalization and externalization studies, and competitive assays were performed. Biodistribution experiments were carried out in normal and tumor-bearing mice. A single product with radiochemical purity >90% and high stability was obtained. In vitro analysis showed specific cellular uptake, IC 50 of 73.2 nM, and a high internalization rate (80%). Biodistribution studies showed low blood and renal uptake and combined hepatobiliary and urinary elimination. Preliminary studies in mice bearing induced breast tumors rendered promising uptake values. K E Y W O R D Sbreast cancer, neuropeptide Y, radiolabeling, scintigraphy, technetium

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Section: Methodsmentioning

confidence: 99%

Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

et al. 2019

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“…The elution profile was as follows: 0 to 3 min, 100% A; 3 to 10 min, linear gradient to 100% B; 10–20 min 100% B. Detection was accomplished with a 1″ × 1″NaI (Tl) crystal scintillation detector (Carta et al., 2014).…”

Section: Methodsmentioning

confidence: 99%

Development and characterization of two novel ⁶⁸Ga‐labelled neuropeptide Y short analogues with potential application in breast cancer imaging

et al. 2021

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In vivo receptor targeting with radiolabelled peptide‐based probes is an attractive approach for the development of novel radiotracers for molecular imaging. This work presents the development and characterization of two novel neuropeptide Y analogues labelled with a positron emitter 68Ga, for potential use in breast cancer imaging. Both analogues share the same amino acid sequence and were derivatized with NOTA through either a lysine linker (L1) or an acetylated lysine (L2). In both cases, a single product with radiochemical purity higher than 95% was obtained. The two complexes were hydrophilic, showed remarkable in vitro stability, good cellular uptake, binding affinity in the nanomolar range and high cellular internalization rate. Biodistribution studies revealed low blood uptake and elimination through the urinary tract. The addition of an acetyl group in the spacer increased the lipophilicity of C2 and modified the reactivity of the ε‐amino group of the lysine which resulted in lower protein binding and lower percentage of injected dose in bladder and urine. The tumour versus muscle ratio was (3.8 ± 0.4) for 68Ga‐L1 and (4.7 ± 0.4) for 68Ga‐L2. These results encourage performing further studies in order to complete the evaluation of both tracers as potential radiopharmaceutical for breast cancer imaging.

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“…+ core is made all the more attractive as a direction for further research by the observation that bis(amido)bis(phosphine) [54] and bis(thioether)bisphosphine) [55] ligands (Figure 4) [57,59,60] or dithiocarboxylates, [61] or unsymmetrical combinations of aminodiphosphine (PNP) with a bidentate thiolate [58,62] or a monodentate tertiary phosphine with a tridentate dithiolate derived from two cysteine residues appended to a peptide ( Figure 5) [63]. The bis(dithiocarbamate) is most simply used as the basis of a divalent targeting agent, such as the bis(bisphosphonate) derivatives developed as potential therapeutic radiopharmaceuticals for bone metastases [60].…”

Section: The [Reo 2 ]mentioning

confidence: 99%

Rhenium-188 Radiochemistry: Challenges and Prospects

Blower¹

2017

Int. J. Nucl. Medi. Res.

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After a lull in development of new chemistry for rhenium-188 and technetium-99m since 2000, there has been new investment in production facilities for Mo-99/Tc-99m coupled with increasing interest in rhenium-188 radionuclide therapy, particularly in developing countries. Much of the chemistry developed in the 1990s is not readily amenable to supporting modern radiopharmaceutical development, which places increased emphasis on molecular targeted radiopharmaceuticals. Consequently there is a need for new radiolabelling chemistry to incorporate these radionuclides into biomolecules using simple, kit-based methodology. This review provides an update on progress towards simple rhenium-188 labelling methods since 2000.

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Assessment of the best N3− donors in preparation of [M(N)(PNP)]-based (M=99mTc-; 188Re) target-specific radiopharmaceuticals: Comparison among succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG600-DTCZ)

Cited by 11 publications

References 24 publications

Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of two novel ⁶⁸Ga‐labelled neuropeptide Y short analogues with potential application in breast cancer imaging

Rhenium-188 Radiochemistry: Challenges and Prospects

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Assessment of the best N3− donors in preparation of [M(N)(PNP)]-based (M=99mTc-; 188Re) target-specific radiopharmaceuticals: Comparison among succinic dihydrazide (SDH), N-methyl-S-methyl dithiocarbazate (HDTCZ) and PEGylated N-methyl-S-methyl dithiocarbazate (HO2C-PEG600-DTCZ)

Cited by 11 publications

References 24 publications

Development and characterization of a 99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of a 99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of two novel 68Ga‐labelled neuropeptide Y short analogues with potential application in breast cancer imaging

Rhenium-188 Radiochemistry: Challenges and Prospects

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Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of a ^99mTc‐labeled Neuropeptide Y short analog with potential application in breast cancer imaging

Development and characterization of two novel ⁶⁸Ga‐labelled neuropeptide Y short analogues with potential application in breast cancer imaging