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School of Life Sciences, University of Dundee

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Article | OPEN Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
University News: `Molecular commando’ identified to tackle hypoxia pathway
School of Life Sciences News: `Molecular commando’ identified to tackle hypoxia pathway
Drug Discovery Today news: `Molecular commando’ identified to tackle hypoxia pathway
New therapeutic target for diseases caused by lack of oxygen
VH298 on the Chemical Probes Portal

Our paper characterising VHL inhibitor VH298 as novel chemical probe of the hypoxia signalling pathway is now published in Nature Communications

  • A visual representation of the crystal structure of the VH298 molecule bound to its target VHL
  • PhD students Julianty and Pedro explained their contributions to the work
  • Figure 1: Biophysical and structural characterization of VH298, a new potent VHL inhibitor.
  • Table 1: Structures and summary of biophysical, permeability and lipophilicity results for VHL inhibitors.
  • Figure 3: VHL inhibitors induce HIF-α transcriptional activity in various cell lines.
  • Figure 4: VH298 elicits a HIF-dependent hypoxic response in various cell lines.
  • Figure 2: VH298 induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines.

Read our open access article here.

Access VH298 from the Chemical Probes portal here.

Prof Alessio Ciulli
Professor of Chemical and Structural Biology
School of Life Sciences, University of Dundee
Division of Biological Chemistry & Drug Discovery
1 James Lindsay Place
Dundee
DD1 5JJ
United Kingdom

E-mail: a.ciulli@dundee.ac.uk
Tel: +44 (0)1382 386230
Fax: +44 (0)1382 386373

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