Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Chao Yang, Wanhe Wang, Linmin Chen, Jiaxin Liang, Sheng Lin, Ming Yuen Lee, Dik Lung Ma*, Chung Hang Leung*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

38 Citations (Scopus)

Abstract

We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL-HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL-HIF1α interaction.

Original languageEnglish
Pages (from-to)12837-12840
Number of pages4
JournalChemical Communications
Volume52
Issue number87
Early online date5 Oct 2016
DOIs
Publication statusPublished - 11 Nov 2016

Scopus Subject Areas

  • Catalysis
  • Electronic, Optical and Magnetic Materials
  • Ceramics and Composites
  • General Chemistry
  • Surfaces, Coatings and Films
  • Metals and Alloys
  • Materials Chemistry

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