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

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

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.

Citation

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. https://doi.org/10.1039/c5dt04706d

• 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
• DOI: https://doi.org/10.1039/c5dt04706d
• Keywords: Ligand design
• Public URL: https://hull-repository.worktribe.com/output/411269
• Publisher URL: http://pubs.rsc.org/en/content/articlelanding/2016/dt/c5dt04706d#!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
• Contract Date: Feb 23, 2016