Tetrazine-<i>trans</i>-cyclooctene ligated lanthanide conjugates for biomedical imaging
File(s)
Author(s)
Type
Journal Article
Abstract
Lanthanide chelates and copper-free ‘click’ chemistry have important uses for targeted molecular imaging and therapeutic strategies. Herein, we report the complexation of lanthanides to a tetrazine-functionalised DO3A macrocyclic chelator and the tetrazine-TCO ligation between the lanthanide(DO3A-tetrazine) complexes and a TCO-PEG4-functionalised rhodamine as a model agent. The luminescent and magnetic properties of the resultant dual-modal conjugates are described. The tetrazine moiety was found to sensitise terbium luminescence, resulting in a ‘turn-off’ effect upon its transformation to the dihydropyridazine linker, with the rhodamine moiety then dominating the fluorescence emissions. The T1 relaxivities of Gd(DO3A-tetrazine) and Gd(DO3A-PEG4-rhodamine) were found to be similar to [Gd(DOTA)]− (Dotarem®). As a proof-of-concept in vivo test, the click conjugates were delivered to mice brains using the combination of focused ultrasound and microbubbles, with neuron uptake of the probes observed.
Date Issued
2026-01-06
Date Acceptance
2025-10-10
Citation
Inorganic Chemistry Frontiers, 2026, 13 (1), pp.63-73
ISSN
2052-1545
Publisher
Royal Society of Chemistry
Start Page
63
End Page
73
Journal / Book Title
Inorganic Chemistry Frontiers
Volume
13
Issue
1
Copyright Statement
© the Partner Organisations 2026. Open Access Article. Published on 14 October 2025. Downloaded on 5/21/2026 12:24:02 PM. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
License URL
Identifier
https://www.ncbi.nlm.nih.gov/pubmed/41132234
PII: d5qi01745a
Subjects
ALDER
Chemistry
Chemistry, Inorganic & Nuclear
CONTRAST AGENTS
CYCLOADDITION
FREE CLICK CHEMISTRY
MICROBUBBLES
Physical Sciences
PROBE
RHODAMINE-B
Science & Technology
SUBSTANCES
SUSCEPTIBILITY
ULTRASOUND
Publication Status
Published
Coverage Spatial
England
Date Publish Online
2025-10-14