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Issue 87, 2016
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Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

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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.

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

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Publication details

The article was received on 13 Jun 2016, accepted on 27 Sep 2016 and first published on 05 Oct 2016


Article type: Communication
DOI: 10.1039/C6CC04938A
Citation: Chem. Commun., 2016,52, 12837-12840
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    Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

    C. Yang, W. Wang, L. Chen, J. Liang, S. Lin, M. Lee, D. Ma and C. Leung, Chem. Commun., 2016, 52, 12837
    DOI: 10.1039/C6CC04938A

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