Nature Communications (Nov 2016)

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

  • Julianty Frost,
  • Carles Galdeano,
  • Pedro Soares,
  • Morgan S. Gadd,
  • Katarzyna M. Grzes,
  • Lucy Ellis,
  • Ola Epemolu,
  • Satoko Shimamura,
  • Marcus Bantscheff,
  • Paola Grandi,
  • Kevin D. Read,
  • Doreen A. Cantrell,
  • Sonia Rocha,
  • Alessio Ciulli

DOI
https://doi.org/10.1038/ncomms13312
Journal volume & issue
Vol. 7, no. 1
pp. 1 – 12

Abstract

Read online

Small molecule probes used to trigger hypoxic response by activating hypoxia inducible factors (HIFs) often lack specificity. Here the authors report a potent small molecule inhibitor that induces hypoxic response by blocking VHL:HIF interactions, providing a selective route to probe hypoxic signalling.