Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

Cancer genome-sequencing studies have revealed a remarkably high prevalence of
mutations in genes encoding subunits of the SWI/SNF chromatin-remodelling complexes …

Small molecule-based targeting of chromatin regulatory factors has emerged as a promising
therapeutic strategy in recent years. The development and ongoing clinical evaluation of …

New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …

Sarcomas are heterogeneous and clinically challenging soft tissue and bone cancers.
Although constituting only 1% of all human malignancies, sarcomas represent the second …

Targeted protein degradation (TPD) mediates protein level through small molecule induced
redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal …

SF3B1 is the most commonly mutated RNA splicing factor in cancer,,–, but the mechanisms
by which SF3B1 mutations promote malignancy are poorly understood. Here we integrated …

Research over the past several decades has unmasked a major contribution of disrupted
chromatin regulatory processes to human disease, particularly cancer. Advances in genome …