Nature Communications (Mar 2016)

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

  • Helena Almqvist,
  • Hanna Axelsson,
  • Rozbeh Jafari,
  • Chen Dan,
  • André Mateus,
  • Martin Haraldsson,
  • Andreas Larsson,
  • Daniel Martinez Molina,
  • Per Artursson,
  • Thomas Lundbäck,
  • Pär Nordlund

DOI
https://doi.org/10.1038/ncomms11040
Journal volume & issue
Vol. 7, no. 1
pp. 1 – 11

Abstract

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Drugs therapeutic efficacy relies on their capability of binding the relevant targets in a physiological environment, which has so far been hard to measure. Here, the authors present a compound library screen based on a target engagement assay that reports on protein stability upon ligands binding in cell.