Kei Mathis

Dec 8, 2023 | nature.com | Mahshid Gazorpak |Karina M. Hugentobler |Pierre-Luc Germain |Miriam Kretschmer |Iryna Ivanova |Kei Mathis | +10 more

AbstractCounteracting the overactivation of glucocorticoid receptors (GR) is an important therapeutic goal in stress-related psychiatry and beyond. The only clinically approved GR antagonist lacks selectivity and induces unwanted side effects. To complement existing tools of small-molecule-based inhibitors, we present a highly potent, catalytically-driven GR degrader, KH-103, based on proteolysis-targeting chimera technology.