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
  • 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.

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