This schematic illustrates the multidimensional optimization strategies for BRD4-targeting PROTACs, encompassing the rational design of the ternary complex, diverse controllable activation systems, and targeted delivery approaches.
In this review we highlight how the synthesis of degraders has evolved in recent years, in particular the application of high-throughput chemistry and screening approaches such as D2B and DEL technologies to expedite discovery timelines.
This feature article highlights the most recent advances in nanoparticle-enabled delivery of proteolysis-targeting chimeras (PROTACs) for spatiotemporally controlled protein degradation.
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.
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.