Dirk Trauner; Joseph A. Flores
Synfacts, 2023, 19(10), 1036
https://doi.org/10.1055/s-0042-1752021

Abstract

DNA-encoded libraries (DELs) represent powerful platforms for identifying small molecule hits in early-stage drug discovery. For hits identified from enrichment data generated with purified protein, methods for triaging ligands based on live cell occupancy would accelerate hit-to-lead prioritization. Here, the authors demonstrate a generalizable workflow to convert DEL hit ligands into bioluminescence resonance energy transfer (BRET) probes for target engagement studies in live cells.