amTCO, a newtrans-cyclooctene derivative to study drug-target interactions in cells

Cécile Echalier, Anna Rutkowska, Ana Kojic, Douglas W. Thomson, Lee J. Edwards, Blandine S.J. McKay, Marcel Mülbaier, Carsten Schultz, Giovanna Bergamini

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

Click chemistry probes have improved the study of drug interactions in live cells and relevant disease models. Proper design of the probes, including the choice of the click moiety coupled to the drug, is crucial to ensure good performance and broad application. A newtrans-cyclooctene derivative, amTCO, was synthesisedviaa novel route using a phthalimide protecting group as a built-in photosensitiser for the cyclooctene isomerization. amTCO improved the physical chemical properties of click chemistry probes compared to standard TCO moieties. An amTCO probe targeting indoleamine 2,3-dioxygenase (IDO1) was a superior tool for visualizing IDO1 and measuring the binding affinities of small molecule inhibitors to IDO1 in cells.

Original languageEnglish (US)
Pages (from-to)1814-1817
Number of pages4
JournalChemical Communications
Volume57
Issue number14
DOIs
StatePublished - Feb 18 2021

ASJC Scopus subject areas

  • Catalysis
  • Electronic, Optical and Magnetic Materials
  • Ceramics and Composites
  • Chemistry(all)
  • Surfaces, Coatings and Films
  • Metals and Alloys
  • Materials Chemistry

Fingerprint Dive into the research topics of 'amTCO, a newtrans-cyclooctene derivative to study drug-target interactions in cells'. Together they form a unique fingerprint.

Cite this