2. Academic Validation
  3. Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α

Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α

  • Angew Chem Int Ed Engl. 2012 Nov 12;51(46):11463-7. doi: 10.1002/anie.201206231.
Dennis L Buckley 1,  Jeffrey L Gustafson,  Inge Van Molle,  Anke G Roth,  Hyun Seop Tae,  Peter C Gareiss,  William L Jorgensen,  Alessio Ciulli,  Craig M Crews
Affiliations

Affiliation

  • 1 Department of Chemistry, Yale University, New Haven, CT 06511, USA.
PMID: 23065727 DOI: 10.1002/anie.201206231
Abstract

E3 ubiquitin ligases, such as the therapeutically relevant VHL, are challenging targets for traditional medicinal chemistry, as their modulation requires targeting protein-protein interactions. We report novel small-molecule inhibitors of the interaction between VHL and its molecular target HIF1α, a transcription factor involved in oxygen sensing.

Figures
Products