Bidirectional modulation of HIF-2 activity through chemical ligands

February 25th, 2019 by Dalei Wu

Bidirectional modulation of HIF-2 activity through chemical ligands

Bidirectional modulation of HIF-2 activity through chemical ligands, Published online: 25 February 2019; doi:10.1038/s41589-019-0234-5

Structural analysis of HIF-2α in complex with agonists and antagonists reveal that chemical ligands regulate the activity of HIF-2α by affecting the stability of the HIF-2α–ARNT heterodimer via redirecting residues in the PAS-B pocket.