Skip to main content

Research Repository

See what's under the surface

Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Kubicek, Vojtech; Bohmova, Zuzana; Price, Thomas W.; Gallo, Juan; Kubíček, Vojtěch; Böhmová, Zuzana; Prior, Timothy J.; Greenman, John; Hermann, Petr; Stasiuk, Graeme J.

Authors

Vojtech Kubicek

Zuzana Bohmova

Thomas W. Price

Juan Gallo

Vojtěch Kubíček

Zuzana Böhmová

Petr Hermann



Abstract

Gallium-68 ( 68 Ga) has been the subject of increasing interest for its potential in the production of radiotracers for diagnosis of diseases. In this work we report the complexation of 68 Ga by the amino acid based tripodal chelate H 3 Dpaa, and two bifunctional derivatives, H 3 Dpaa.dab and H 4 Dpaa.ga, under a range of conditions with particular emphasis on the rapid complexation of 68 Ga at pH 7.4. 100 μM H 3 Dpaa achieved a radiochemical yield of 95% at pH 7.4 in 5 minutes at 37 °C. The bifunctional derivatives H 4 Dpaa.ga and H 3 Dpaa.dab achieved 94% and 84% radiochemical yields, respectively, under the same conditions. The resulting Ga(iii) complexes show thermodynamic stabilities of logK GaDpaa = 18.53, logK GaDpaa.dab = 22.08, logK GaDpaa.ga = 18.36. Unfortunately, the resulting radiolabelled species do not present sufficient serum stability for in vivo application. Herein we show a flexible synthesis for bifunctional chelators based on amino acids that rapidly complex 68 Ga under physiological conditions.

Journal Article Type Article
Publication Date Nov 17, 2017
Journal Dalton Transactions
Print ISSN 1477-9226
Electronic ISSN 1477-9234
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Volume 46
Issue 48
Pages 16973-16982
Institution Citation Kubicek, V., Bohmova, Z., Price, T. W., Gallo, J., Kubíček, V., Böhmová, Z., …Stasiuk, G. J. (2017). Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH. Dalton transactions : an international journal of inorganic chemistry / RSoC, 46(48), 16973-16982. https://doi.org/10.1039/c7dt03398b
DOI https://doi.org/10.1039/c7dt03398b
Keywords Inorganic Chemistry
Copyright Statement ©2018 The University of Hull.

This is the accepted version of an article published in Dalton Transactions. The published version is available at the DOI above.
Additional Information : This document is Similarity Check deposited; : Supplementary Information; : Crystal Structure Data; : Juan Gallo (ORCID); : Vojtěch Kubíček (ORCID); : Vojtěch Kubíček (ResearcherID); : Timothy J. Prior (ORCID); : John Greenman (ORCID); : Petr Hermann (ORCID); : Petr Hermann (ResearcherID); : Graeme J. Stasiuk (ORCID); : Single-blind; : Received 12 September 2017; Accepted 16 November 2017; Accepted Manuscript published 17 November 2017; Advance Article published 27 November 2017; Version of Record published 12 December 2017

Files

Article (423 Kb)
PDF

Copyright Statement
©2018 The University of Hull.

This is the accepted version of an article published in Dalton Transactions. The published version is available at the DOI above.





You might also like



Downloadable Citations