Real-Time Multi-Photon Tracking and Bioimaging of Glycosylated Theranostic Prodrugs upon Specific Enzyme Triggered Release

Elena Calatrava-Pérez, Luke A. Marchetti, Gavin J. McManus, Dylan M. Lynch, Robert B. P. Elmes, D. Clive Williams, Thorfinnur Gunnlaugsson (Lead / Corresponding author), Eoin M. Scanlan (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

Abstract

Real-time tracking of prodrug uptake, delivery and activation in vivo represents a major challenge for prodrug development. Herein, we demonstrate the use of novel glycosylated theranostics of the cancer pharmacophore Amonafide in highly-selective, enzymatic triggered release. We show that the use of endogenous enzymes for activated release of the therapeutic component can be observed, in real time, and monitored using one and two-photon bioimaging, offering unique insight into the prodrug pharmacokinetic profile. Furthermore, we demonstrate that the potent cytotoxicity of Amonafide is preserved using this targeted approach.

Original languageEnglish
Article numbere202103858
Number of pages7
JournalChemistry - A European Journal
Volume28
Issue number3
Early online date24 Nov 2021
DOIs
Publication statusPublished - 13 Jan 2022

Keywords

  • antitumor agents
  • carbohydrates
  • glycosidase
  • imaging agents
  • prodrugs

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