Design, synthesis, and preclinical evaluation of a novel bifunctional macrocyclic chelator for theranostics of cancers

Xu, Jianfeng; Cai, Fei; Luo, Zhigang; Fan, Wei; Dai, Juan; Cui, Jingjing; Li, Shihong; Geng, Changran; Zheng, Qi‐Huang; Wang, Zheng; Tang, Xiaobin

doi:10.1007/s00259-022-05750-8

Cited by 3 publications

(6 citation statements)

References 38 publications

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“…150 (B) Comparative PET imaging studies of 68 Ga-labeled-PSMA-617 (left panel), 177 Lu-labeled-PSMA-617 (middle panel), and 89 Zr-labeled-KN035 (right panel) in LNCaP tumor-bearing nude mice at different time points. 151 Reproduced with permission. 150 Copyright 2016, Wiley.…”

Section: Zirconium-89mentioning

confidence: 99%

Section: Zirconium-89mentioning

confidence: 99%

“…Xu et al reported a new bifunctional chelating agent, Dar, containing multiple donors such as pyridine nitrogen, aliphatic nitrogen, and phenolic oxygen. 151 Dar-PSMA-617 complexes were successfully labeled with 68 Ga, 89 Zr, and 177 Lu at room temperature with high RCY and purity. In vitro and in vivo data demonstrated that radiolabeled-Dar-PSMA-617 exhibited comparable, or even better, tumor uptake and antitumor efficacy with radiolabeled-DOTA/DFO-PSMA-617 (Figure 9B).…”

Section: Zirconium-89mentioning

confidence: 99%

“…Xu et al. reported a new bifunctional chelating agent, Dar, containing multiple donors such as pyridine nitrogen, aliphatic nitrogen, and phenolic oxygen 151 . Dar‐PSMA‐617 complexes were successfully labeled with 68 Ga, 89 Zr, and 177 Lu at room temperature with high RCY and purity.…”

Section: Zirconium‐89mentioning

confidence: 99%

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Advances in macrocyclic chelators for positron emission tomography imaging

Wang²,

Kong

et al. 2023

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In recent years, radiometals have been successfully applied to medicine because of their breadth of decay properties and increased production and availability. Bifunctional chelators play a key role in radiometal‐based radiopharmaceuticals, affecting the labeling, targeting, and pharmacokinetics of bioconjugations and ensuring the stable complexation of the metal in vivo. The capacity of macrocycles to form complexes with extremely high thermodynamics, kinetics, and stability compared to acyclic chelators continues to pique the curiosity of pharmacists and biochemists among all prospective chelators utilized for the radiometal chelation. As new imaging modalities and therapeutic targets develop, the discovery of novel ligand structures with suitable chemical and biological features encourages the modification of chelators with charge and chemical properties. Herein, we present a comprehensive review of developments of macrocyclic chelators for PET radiopharmaceuticals, including innovative chelating agents with new structures and known chelating agent modifications, and their physical‐chemical properties, as well as their biological characteristics and applications in vivo.

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Section: Zirconium-89mentioning

confidence: 99%

Section: Zirconium-89mentioning

confidence: 99%

Section: Zirconium-89mentioning

confidence: 99%

Section: Zirconium‐89mentioning

confidence: 99%

See 2 more Smart Citations

Advances in macrocyclic chelators for positron emission tomography imaging

Wang²,

Kong

et al. 2023

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“…Theranostic systems compatible with radiometals of different elements are being explored using discrete chelators with capacity for cross-metal binding. [10][11][12][13][14] We have taken a different approach by graing together two chelators, desferrioxamine B (DFOB, 1) and 1,4,7,10tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA, 2) (Chart 1), which have been established experimentally and/or clinically as useful chelators for 89 Zr(IV) (positron-emission tomography (PET) imaging) or 177 Lu(III) (b-radiation therapy), respectively.…”

Section: Introductionmentioning

confidence: 99%