Skip to main content
. Author manuscript; available in PMC: 2014 Feb 28.
Published in final edited form as: J Med Chem. 2013 Feb 18;56(4):1739–1747. doi: 10.1021/jm301847z

Figure 1.

Figure 1

Basis of small molecule regulation of protein-protein interactions in HIF-2. A) Crystal structure of the HIF-2α–ARNT PAS-B heterodimer9b (PDB code: 3F1P), highlighting the internal cavity within HIF-2α PAS-B (grey surface, internal waters represented as red spheres). Sidechains lining the cavity are provided by a mix of hydrophobic and polar residues as shown. B) Schematic for small molecule regulation of HIF-2, with ligand binding to the HIF-2α PAS-B cavity, distorting the adjacent β-sheet that also provides the ARNT PAS-B binding surface.7