Issue 40, 2016

Current advances in ligand design for inorganic positron emission tomography tracers 68Ga, 64Cu, 89Zr and 44Sc

Abstract

A key part of the development of metal based Positron Emission Tomography probes is the chelation of the radiometal. In this review the recent developments in the chelation of four positron emitting radiometals, 68Ga, 64Cu, 89Zr and 44Sc, are explored. The factors that effect the chelation of each radio metal and the ideal ligand system will be discussed with regards to high in vivo stability, complexation conditions, conjugation to targeting motifs and complexation kinetics. A series of cyclic, cross-bridged and acyclic ligands will be discussed, such as CP256 which forms stable complexes with 68Ga under mild conditions and PCB-TE2A which has been shown to form a highly stable complex with 64Cu. 89Zr and 44Sc have seen significant development in recent years with a number of chelates being applied to each metal – eight coordinate di-macrocyclic terephthalamide ligands were found to rapidly produce more stable complexes with 89Zr than the widely used DFO.

Graphical abstract: Current advances in ligand design for inorganic positron emission tomography tracers 68Ga, 64Cu, 89Zr and 44Sc

Article information

Article type
Perspective
Submitted
19 صفر 1437
Accepted
24 ربيع الثاني 1437
First published
24 ربيع الثاني 1437

Dalton Trans., 2016,45, 15702-15724

Author version available

Current advances in ligand design for inorganic positron emission tomography tracers 68Ga, 64Cu, 89Zr and 44Sc

T. W. Price, J. Greenman and G. J. Stasiuk, Dalton Trans., 2016, 45, 15702 DOI: 10.1039/C5DT04706D

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