The paper optimizes and evaluates two cell-based assays for degrader discovery, finding that the signal rescue assay reliably identifies active degraders and filters out non-specific compounds.

ACS Pharmacology & Translational Science · Jul 20, 2025Peer-reviewedPharmacology & Toxicology

STRUCTURE-BASED DESIGN OF PROTACS FOR THE DEGRADATION OF SOLUBLE EPOXIDE HYDROLASE

Julia Schönfeld, Steffen Brunst, Ludmila Ciomirtan, Lena Willmer, Michel André Chromik, Adarsh M. Kumar, Timo Frömel, Nick Liebisch, Arne Hackspacher, Johanna H. M. Ehrler, Lukas Wintermeier, Christina Hesse, Jan Fiedler, Jan Heering, Hinrich Freitag, , Kerstin Hiesinger

This paper designs and tests sEH-PROTACs to degrade soluble epoxide hydrolase, identifying PROTAC 23 as effective in degrading sEH in human macrophages.

Journal of Medicinal Chemistry · Jun 18, 2025Peer-reviewedBiochemistry

Click Chemistry Enables Rapid Development of Potent sEH PROTACs Using a Direct-to-Biology Approach

Julia Schönfeld, Nick Liebisch, Steffen Brunst, Lilia Weizel, Stefan Knapp, Aimo Kannt, Ewgenij Proschak, Kerstin Hiesinger

This paper develops a miniaturized Direct-to-Biology platform for rapid PROTAC degrader synthesis and screening, identifying potent sEH degraders with subnanomolar activity.

Chemical Communications · Jan 1, 2025Peer-reviewedCell Biology