Chemical biology tools to modulate protein levels in cells are critical to decipher complex
biology. Targeted protein degradation offers the potential for rapid and dose-dependent …

Targeted protein degradation is an emerging technology that can be used for modulating the
activity of epigenetic protein targets. Among bromodomain-containing proteins, a number of …

Targeted protein degradation is a powerful induced-proximity tool to control cellular protein
concentrations using small molecules. However, the design of selective degraders remains …

Targeted protein degradation with monovalent molecular glue degraders is a powerful
therapeutic modality for eliminating disease causing proteins. However, rational design of …

Abstract The BET proteins BRD2, BRD3, and BRD4 play important roles in transcriptional
regulation and can be degraded by proteolysis-targeting chimeras (PROTACs) for BET …

Ligand-induced target protein degradation has emerged as a promising therapeutic
strategy, particularly in cancer, but efforts so far have often been limited by various factors …

Starting from a nonselective bromodomain and extraterminal (BET) inhibitor and a cereblon
ligand, we have used precise conformational control for the development of two potent and …

The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule
approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 …

Engineered destruction of target proteins by recruitment to the cell's degradation machinery
has emerged as a promising strategy in drug discovery. The majority of molecules that …

Proteolysis targeting chimeras (PROTACs) are complex molecules to design and optimize
as degraders, primarily because the linker that bridges the two binding ligands is a highly …