Daniel Längle, Stephanie Wojtowicz-Piotrowski, Till Priegann, Niklas Keller, Fabian Wesseler, Elena S Reckzeh, Karsten Steffens, Christoph Grathwol, Jana Lemke, Maren Flasshoff, Christian Näther, Anna C Jonson, Andreas Link, Oliver Koch, Gianni M Di Guglielmo, Dennis Schade
The TGFβ type II receptor (TβRII) is a central player in all TGFβ signaling downstream events, has been linked to cancer progression, and thus, has emerged as an auspicious anti-TGFβ strategy. Especially its targeted degradation presents an excellent goal for effective TGFβ pathway inhibition. Here, cellular structure-activity relationship (SAR) data from the TβRII degrader chemotype 1 was successfully transformed into predictive ligand-based pharmacophore models that allowed scaffold hopping...
April 12, 2024: ACS Pharmacology & Translational Science