Emerging chelators for nuclear imaging

Sneddon, Deborah; Cornelissen, Bart

doi:10.1016/j.cbpa.2021.03.001

Cited by 29 publications

(32 citation statements)

References 78 publications

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“…A solution of [Cu(L)] (c = 30 mM) in 0.4 M NH 3 /HCl buffer (pH 9.0) or in 0.1 M KOH (pH 13.0) was incubated in a firmly closed NMR tube at room temperature. 1 H NMR measurements were run regularly using 0.1 % tBuOH in D 2 O in an insert tube as a standard. Hydrolysis of the amide bond in Cu II -H 2 L 2 complex was evaluated by integrating the triplet signal of the CH 3 group from free diethylamine with respect to an external standard and quantified by standard addition of diethylamine.…”

Section: Methodsmentioning

confidence: 99%

“…Current molecular imaging and nuclear medicine increasingly apply several metal radioisotopes as radiotracers in Positron Emission Tomography (PET) and Single-Photon Emission Computed Tomography (SPECT) or in radiotherapy. [1][2][3][4] Among the most commonly used metal radioisotopes, copper radioisotopes (mainly 64 Cu and 67 Cu) stand out for their suitable radiochemical properties and their increasing availability and decreasing price. [5][6][7][8] They can be used for both PET imaging (β + emitters 61 Cu or 64 Cu) and therapy (β À emitter 67 Cu), and as isotopes of the same element, such imaging and therapeutic tracers can form the "ideal"/"matched" theranostic pair.…”

Section: Introductionmentioning

confidence: 99%

“…These derivatives bear various coordinating pendant arms, e. g. acetate arms in their parent ligand, 1,4,7-triazacyclononane-1,4,7-triacetic acid (H 3 nota, Scheme 1). [1][2][3][9][10][11] However, several tacn derivatives with other coordinating pendant arms have been investigated as chelators for copper radionuclides. [1][2][3][4][5][6][7][8][9][12][13][14][15][16][17][18][19][20] Complexes of H 3 nota, as highly hydrophilic and lowmolecular-weight compounds, show a non-specific uptake in organs and a fast body clearance.…”

Section: Introductionmentioning

confidence: 99%

“…These derivatives bear various coordinating pendant arms, e. g. acetate arms in their parent ligand, 1,4,7‐triazacyclononane‐1,4,7‐triacetic acid (H 3 nota, Scheme 1). [1–3,9–11] However, several tacn derivatives with other coordinating pendant arms have been investigated as chelators for copper radionuclides [1–9,12–20] …”

Section: Introductionmentioning

confidence: 99%

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Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study

et al. 2022

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NOTA monoamides are commonly and widely used chelators for the complexation of copper radioisotopes applied in molecular imaging and targeted nuclear therapy. However, information about their coordination behavior remains scarce. In this study, two NOTA‐monoamides, N‐ethyl (H2L1) and N,N‐diethyl (H2L2), were synthesized as model ligands and tested to probe differences in their coordination behavior between the secondary and tertiary amide pendant arms for potential applications as copper radioisotope carriers. Our results demonstrated that the solid [Cu(L1)] and [Cu(L2)] complex have a distorted octahedral arrangement, similar to structure of the [Cu(Hnota)] complex. As shown by equilibrium data, the ligands have a slightly lower basicity, and thus complexes with divalent metal ions and LiI have slightly lower stability constants than those of the parent ligand, H3nota. The dissociation constants of the CuII, ZnII and NiII complexes with H2L1 also indicate deprotonation and N‐coordination of the secondary amide group at pH>9. Complexation of CuII ions with the title ligands is slower than that with H3nota but still very fast (quantitative binding in <1 s, pH 2, millimolar concentrations), and CuII complexes of both monoamide ligands are more resistant to acid‐assisted decomplexation than the CuII‐H3nota complex. Therefore, our coordination data highlight that NOTA‐monoamides are suitable chelators for molecular imaging and nuclear medicine.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study

et al. 2022

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“…Table 2 shows some of the commonly used therapeutic radionuclides [5,6,16]. For common chelators, the properties of metallic radionuclides and the corresponding radiopharmaceuticals, readers could refer to review articles by Vermeulen, Kostelnik, Boros and Sneddon [5,6,8,17].…”

Section: The General Structure Of Targeted Metal-based Radiopharmaceuticalsmentioning

confidence: 99%

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Zhou¹,

Dong²,

Shen

2021

Molecules

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Hydroxypyridinones (HOPOs) have been used in the chelation therapy of iron and actinide metals. Their application in metal-based radiopharmaceuticals has also been increasing in recent years. This review article focuses on how multidentate HOPOs can be used in targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals. The general structure of radiometal-based targeted radiopharmaceuticals, a brief description of siderophores, the basic structure and properties of bidentate HOPO, some representative HOPO multidentate chelating agents, radiopharmaceuticals based on HOPO multidentate bifunctional chelators for gallium-68, thorium-227 and zirconium-89, as well as the future prospects of HOPO multidentate bifunctional chelators in other metal-based radiopharmaceuticals are described and discussed in turn. The HOPO metal-based radiopharmaceuticals that have shown good prospects in clinical and preclinical studies are gallium-68, thorium-227 and zirconium-89 radiopharmaceuticals. We expect HOPO multidentate bifunctional chelators to be a very promising platform for building novel targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals.

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Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents

Kubeil,

Suzuki,

Casulli

et al. 2023

Adv Healthcare Materials

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Nanogels open up access to a wide range of applications and offer among others hopeful approaches for use in the field of biomedicine. This review provides a brief overview of current developments of nanogels in general, particularly in the fields of drug delivery, therapeutic applications, tissue engineering and sensor systems. Specifically, cyclodextrin (CD)‐based nanogels are important because they have exceptional complexation properties and are highly biocompatible. Nanogels as a whole and CD‐based nanogels in particular can be customized in a wide range of sizes and equipped with a desired surface charge as well as containing additional molecules inside and outside, such as dyes, solubility‐mediating groups or even biological vector molecules for pharmaceutical targeting. Currently, biological investigations are mainly carried out in vitro, but more and more in vivo applications are gaining importance. Modern molecular imaging methods are increasingly being used for the latter. Due to an extremely high sensitivity and the possibility of obtaining quantitative data on pharmacokinetic and pharmacodynamic properties, nuclear methods such as single photon emission computed tomography (SPECT) and positron emission tomography (PET) using radiolabeled compounds are particularly suitable here. The use of radiolabeled nanogels for imaging, but also for therapy, is being discussed.This article is protected by copyright. All rights reserved

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Emerging chelators for nuclear imaging

Cited by 29 publications

References 78 publications

Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study

Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents

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Emerging chelators for nuclear imaging

Cited by 29 publications

References 78 publications

Complexes of NOTA‐Monoamides with CuII Ions: Structural, Equilibrium, and Kinetic Study

Complexes of NOTA‐Monoamides with CuII Ions: Structural, Equilibrium, and Kinetic Study

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents

Contact Info

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Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study

Complexes of NOTA‐Monoamides with Cu^II Ions: Structural, Equilibrium, and Kinetic Study