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. Author manuscript; available in PMC: 2017 Jul 6.
Published in final edited form as: Nature. 2016 Sep 5;539(7627):107–111. doi: 10.1038/nature19795

Extended Data Figure 1. Binding of PT2399 to PAS-B domain of human HIF2α as determined by X-Ray co-crystal structure.

Extended Data Figure 1

a, X-Ray co-crystal of PT2399 (magenta) bound to HIF2α/ARNT PAS-B domains (ARNT removed for clarity). b, X-Ray co-crystal of PT2399 (magenta) with HIF2α/ARNT PAS-B domains (zoomed in on HIF2α PAS-B pocket). c, Immunoblots of anti-ARNT1 immunoprecipitates (IP) of Hep3B cells treated with PT2399 or DMSO. d, Immunoblot of 786-O cells expressing shRNA against HIF2α (3806) or control shRNA. e, HIF2α specific gene regulation in Hep3B; n=3 biological replicates. f, Immunoblot analysis (top) and quantification (bottom) of HIF2α in 786-O cells treated with DMSO or PT2399 for 16 hours and then exposed to cycloheximide for the indicated time periods; n=3 biological replicates. g, Enrichment plots for representative gene sets previously linked to HIF, hypoxia, or c-Myc. h, i, Plasma PT2399 levels after administration of a single dose of PT2399 to CD-1 mice; n=3 per time point from one experiment.