Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …

BET proteins, which influence gene expression and contribute to the development of cancer,
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …

PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules consisting of
two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a …

Epigenetic dysregulation has long been recognized as a key factor contributing to
tumorigenesis and tumour maintenance that can influence all of the recognized hallmarks of …

Proteins of the bromodomain and extra-terminal (BET) domain family are epigenetic readers
that bind acetylated histones through their bromodomains to regulate gene transcription …

Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …

Prostate cancer has the second highest incidence among cancers in men worldwide and is
the second leading cause of cancer deaths of men in the United States. Although androgen …

Cancer Stem Cells Cancers arise in tissues that can replicate and self-renew. Like normal
tissues, cancers can replenish themselves, grow, and metastasize because of stem cells that …

Bromodomains (BRDs) are evolutionarily conserved protein–protein interaction modules
that are found in a wide range of proteins with diverse catalytic and scaffolding functions and …

BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive
target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have …