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

D.L. Buckley, J.L. Gustafson, I. Van-Molle, A.G. Roth, H.S. Tae, P.C. Gareiss, W.L. Jorgensen, Alessio Ciulli, C.M. Crews

    Research output: Contribution to journalArticlepeer-review

    49 Citations (Scopus)

    Abstract

    By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1a, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC50 value of 0.9-µM and is thus the first sub-micromolar inhibitor of the VHL-HIF1a interaction.

    Original languageEnglish
    Pages (from-to)11463-11467
    Number of pages5
    JournalAngewandte Chemie International Edition
    Volume51
    Issue number46
    DOIs
    Publication statusPublished - 12 Nov 2012

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