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

Price, Thomas W.; Greenman, John; Stasiuk, Graeme J.


Thomas W. Price

Graeme J. Stasiuk


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.


Price, T. W., Greenman, J., & Stasiuk, G. J. (2016). Current advances in ligand design for inorganic positron emission tomography tracers ⁶⁸Ga, ⁶⁴Cu, ⁸⁹Zr and ⁴⁴Sc. Dalton Transactions : an international journal of inorganic chemistry, 45(40), 15702-15724.

Journal Article Type Article
Acceptance Date Feb 3, 2016
Online Publication Date Feb 3, 2016
Publication Date Feb 3, 2016
Deposit Date Feb 23, 2016
Publicly Available Date Feb 23, 2016
Journal Dalton transactions
Print ISSN 1477-9226
Electronic ISSN 1477-9234
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Volume 45
Issue 40
Pages 15702-15724
Keywords Ligand design
Public URL
Publisher URL!divAbstract
Additional Information : This document is Similarity Check deposited; : The Royal Society of Chemistry has an exclusive publication licence for this journal; OPEN ACCESS: The accepted version of this article will be made freely available after a 12 month embargo period; : Single-blind; : Received 1 December 2015; Accepted 3 February 2016; Accepted Manuscript published 3 February 2016; Advance Article published 11 February 2016; Version of Record published 12 October 2016


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