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Durham University

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Publication details for Prof. David Parker

Starck, Matthieu, Fradgley, Jack D., Di Vita, Stefania, Mosely, Jackie, Pal, Robert & Parker, David (2020). Targeted Luminescent Europium Peptide Conjugates: Comparative Analysis Using Maleimide and para-Nitropyridyl Linkages for Organelle Staining. Bioconjugate Chemistry 31(2): 229-240.

Author(s) from Durham

Abstract

The syntheses and photophysical behaviour of nine, strongly luminescent nonadentate
Eu(III) complexes are reported. Each complex is based on N-functionalised 1,4,7-
triazacyclononane, and linkage to other groups or targeting vectors can occur either via
amide bond formation to a coordinated pyridine p-aminopropyl group or via a nucleophilic
substitution reaction involving thiol attack on a metal coordinated p-nitropyridyl moiety.
Evidence is presented in favour of the latter conjugation strategy, as parallel work with
maleimide conjugates was complicated or compromised by the propensity to undergo postconjugation thiol exchange or succinimide ring hydrolysis reactions. Confocal microscopy
and spectral imaging studies revealed that the peptide conjugate of AcCFFKDEL was found to
localise selectively in the endoplasmic reticulum of mouse fibroblast cells, whereas the
related maleimide conjugate was only observed in cellular lysosomes