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.
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Yang et al. (2016) studied this question.
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