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Demonstrates inhibition of hypoxia-regulated gene expression in HIF-2α inhibitors, highlighting potential clinical applications.
difluorination was critical for productive engagement of the lipophilic pocket, with hyperconjugative effects contributing to improved binding efficiency and facial polarization enhancing physicochemical properties. These features translated into improved biochemical and cellular activity, including inhibition of hypoxia-regulated gene expression. Insights from this campaign ultimately informed the discovery of casdatifan, a clinical-stage HIF-2α inhibitor, underscoring the translational potential of this novel chemotype.
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Mata et al. (2026) studied this question.
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