dTRIM24, a conjugate of IACS-9571 a TRIM24 bromodomain ligand and VL-269 a VHL E3 ubiquitin ligase ligand, is a selective bifunctional degrader of bromodomain-containing transcriptional regulator TRIM24 (transcriptional intermediary factor 1a). dTRIM24 induces rapid and sustain proteasome degradation of TRIM24 in 293FT cells.
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Nature chemical biology, 14(4), 405-412 (2018-03-07)
The addressable pocket of a protein is often not functionally relevant in disease. This is true for the multidomain, bromodomain-containing transcriptional regulator TRIM24. TRIM24 has been posited as a dependency in numerous cancers, yet potent and selective ligands for the
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