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核心技术专利：CN118964589B侵权必究
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作为正电子发射断层显像（PET）放射性核素锆-89螯合剂的双大环对苯二甲酰胺配体

Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89.

作者信息

Pandya Darpan N, Pailloux Sylvie, Tatum David, Magda Darren, Wadas Thaddeus J

机构信息

Radiochemistry Service and Cyclotron Operations, Cancer Biology and Radiology, Wake Forest School of Medicine, Medical Center Blvd., Winston-Salem, NC 27157, USA.

出版信息

Chem Commun (Camb). 2015 Feb 11;51(12):2301-3. doi: 10.1039/c4cc09256b.

DOI:10.1039/c4cc09256b
PMID:25556851
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4507282/
Abstract

The development of bifunctional chelators (BFCs) which can stably chelate zirconium-89 ((89)Zr) while being conjugated to targeting molecules is an area of active research. Herein we report the first octadentate terephthalamide ligands, which are easily radiolabeled with (89)Zr and are highly stable in vitro. They represent a novel class of chelators, which are worthy of further development as BFCs for (89)Zr.

摘要

能够在与靶向分子偶联的同时稳定螯合锆-89（89Zr）的双功能螯合剂（BFCs）的开发是一个活跃的研究领域。在此，我们报道了首例八齿对苯二甲酰胺配体，它们易于用89Zr进行放射性标记且在体外高度稳定。它们代表了一类新型螯合剂，作为用于89Zr的BFCs值得进一步开发。

相似文献

[1]
Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89.

Chem Commun (Camb). 2015-2-11

[2]
Evaluation of macrocyclic hydroxyisophthalamide ligands as chelators for zirconium-89.

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[3]
Design, synthesis and evaluation of novel bifunctional tetrahydroxamate chelators for PET imaging of Zr-labeled antibodies.

Bioorg Med Chem Lett. 2017-2-15

[4]
Rational Design, Development, and Stability Assessment of a Macrocyclic Four-Hydroxamate-Bearing Bifunctional Chelating Agent for Zr.

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[5]
An octadentate bifunctional chelating agent for the development of stable zirconium-89 based molecular imaging probes.

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[6]
Comparison of the octadentate bifunctional chelator DFO*-pPhe-NCS and the clinically used hexadentate bifunctional chelator DFO-pPhe-NCS for Zr-immuno-PET.

Eur J Nucl Med Mol Imaging. 2017-2

[7]
Alternative chelator for ⁸⁹Zr radiopharmaceuticals: radiolabeling and evaluation of 3,4,3-(LI-1,2-HOPO).

J Med Chem. 2014-5-19

[8]
Radiolabelling of the octadentate chelators DFO* and oxoDFO* with zirconium-89 and gallium-68.

J Biol Inorg Chem. 2020-8

[9]
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Inorg Chem. 2023-12-18

[10]
Rational Design, Synthesis and Preliminary Evaluation of Novel Fusarinine C-Based Chelators for Radiolabeling with Zirconium-89.

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引用本文的文献

[1]
Zirconium 89 and Copper 64 for ImmunoPET: From Antibody Bioconjugation and Radiolabeling to Molecular Imaging.

Pharmaceutics. 2024-6-30

[2]
Bifunctional octadentate pseudopeptides as Zirconium-89 chelators for immuno-PET applications.

EJNMMI Radiopharm Chem. 2024-5-6

[3]
The Race for Hydroxamate-Based Zirconium-89 Chelators.

Cancers (Basel). 2021-9-4

[4]
Polyazamacrocycle Ligands Facilitate Zr Radiochemistry and Yield Zr Complexes with Remarkable Stability.

Inorg Chem. 2020-11-10

[5]
A High-Denticity Chelator Based on Desferrioxamine for Enhanced Coordination of Zirconium-89.

Inorg Chem. 2020-8-17

[6]
Direct comparison of the in vitro and in vivo stability of DFO, DFO* and DFOcyclo* for Zr-immunoPET.

Eur J Nucl Med Mol Imaging. 2019-6-3

[7]
Rational Design, Synthesis and Preliminary Evaluation of Novel Fusarinine C-Based Chelators for Radiolabeling with Zirconium-89.

Biomolecules. 2019-3-6

[8]
A comprehensively revised strategy that improves the specific activity and long-term stability of clinically relevant Zr-immuno-PET agents.

Dalton Trans. 2018-9-4

[9]
Evaluation of a chloride-based Zr isolation strategy using a tributyl phosphate (TBP)-functionalized extraction resin.

Nucl Med Biol. 2018-6-18

[10]
Recent Advances in Zirconium-89 Chelator Development.

Molecules. 2018-3-12

本文引用的文献

[1]
Tripodal tris(hydroxypyridinone) ligands for immunoconjugate PET imaging with (89)Zr(4+): comparison with desferrioxamine-B.

Dalton Trans. 2015-3-21

[2]
⁸⁹Zr-huJ591 immuno-PET imaging in patients with advanced metastatic prostate cancer.

Eur J Nucl Med Mol Imaging. 2014-11

[3]
An octadentate bifunctional chelating agent for the development of stable zirconium-89 based molecular imaging probes.

Chem Commun (Camb). 2014-10-9

[4]
Alternative chelator for ⁸⁹Zr radiopharmaceuticals: radiolabeling and evaluation of 3,4,3-(LI-1,2-HOPO).

J Med Chem. 2014-5-19

[5]
Charting the mechanism and reactivity of zirconium oxalate with hydroxamate ligands using density functional theory: implications in new chelate design.

Dalton Trans. 2014-7-14

[6]
Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.

J Nucl Med. 2013-4-11

[7]
Investigation of Zr(IV) and 89Zr(IV) complexation with hydroxamates: progress towards designing a better chelator than desferrioxamine B for immuno-PET imaging.

Chem Commun (Camb). 2012-12-19

[8]
Annotating MYC status with 89Zr-transferrin imaging.

Nat Med. 2012-9-23

[9]
Targeting the internal epitope of prostate-specific membrane antigen with 89Zr-7E11 immuno-PET.

J Nucl Med. 2011-9-9

[10]
Magnitude of enhanced permeability and retention effect in tumors with different phenotypes: 89Zr-albumin as a model system.

J Nucl Med. 2011-3-18

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