Application of HIV-1 viral protein R-derived-peptides as new E3 ligase-binding components of BRD4 degraders.

ABSTRACT: Proteolysis targeting chimeras (PROTACs) have become a new modality for drug development of particular importance for cancer chemotherapy. PROTACs are composed of a ligand that binds to the protein of interest (POI) tethered by a linker to a ubiquitin E3 ligase-binding motif. These molecules can degrade the POI by ubiquitination and subsequent digestion using the ubiquitin-proteasome system (UPS). Although more than six hundred E3 ligases are encoded in human genome, only a small number are currently utilized by PROTACs. Because the expression levels and activities of E3 ligases vary among the cell lines, it can be advantageous to develop PROTACs that utilize new E3 ligase-binding components. In our current work we report new E3 ligase-binding ligands that employ viral protein R (Vpr), an

SUBMITTER: Tsuji K 

PROVIDER: S-EPMC12569793 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature