Bromodomain-containing proteins are key epigenetic regulators of gene transcription and
readers of the histone code. However, the therapeutic benefits of modulating this target class …

Targeted protein degradation via cereblon (CRBN), a substrate receptor of an E3 ubiquitin
ligase complex, is an increasingly important strategy in various clinical settings, in which the …

Manipulation of the ubiquitin–proteasome system to achieve targeted degradation of
proteins within cells using chemical tools and drugs has the potential to transform …

Proteolysis-Targeting Chimeras (PROTACs) are bifunctional molecules that bring a target
protein and an E3 ubiquitin ligase into proximity to append ubiquitin, thus directing target …

Small molecule degraders of disease-driving proteins offer a clinically proven modality with
enhanced therapeutic efficacy and the potential to tackle previously undrugged targets …

Thalidomide, pomalidomide and lenalidomide, collectively referred to as immunomodulatory
imide drugs (IMiDs), are frequently employed in proteolysis‐targeting chimeras (PROTACs) …

Targeted protein degradation has arisen as a powerful strategy for drug discovery allowing
the targeting of undruggable proteins for proteasomal degradation. This approach most …

Targeted protein degradation (TPD) and proteolysis-targeting chimeras (PROTACs) have
arisen as powerful therapeutic modalities for degrading specific proteins in a proteasome …

Post-translationally appended acetyllysine marks on histone tails are key regulatory features
of the epigenetic code. Bromodomains are “readers” of this specific lysine acetylation code …

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …