A systematic investigation of cyclic imide stereoisomers in small molecules, peptides, and proteins, examining their racemization, CRBN engagement, ternary complex formation in vitro, and resulting degradation outcomes in cells.
PROTAC–Pt(IV) represents a new class of dual-action Pt(IV) prodrugs integrating platinum drugs with PROTAC-mediated protein degradation, exhibiting superior antitumor efficacy compared to conventional Pt(IV) prodrug and PROTAC alone in vivo.
This review discusses leveraging click chemistry to address unmet needs in PROTAC development.
An HIV-1 accessory protein Vpr-derived peptide functions as an E3 ligase ligand, and this peptide-containing molecules successfully degraded their target protein, BRD4. These molecules also showed HIV-1 latency reversing activity.
This review summarizes the past and present advances in developing degraders of epigenetic targets which play critical roles in many crucial biological pathways and therefore, targeted for the discovery of therapeutics.