Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …

Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …

We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …

The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …

Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …

Proteolysis targeting chimera (PROTAC) degradation of pathogenic proteins by hijacking of
the ubiquitin-proteasome-system has become a promising strategy in drug design. The …

We report small molecular PROTAC compounds targeting the androgen receptor N-terminal
domain (AR-NTD), which were obtained by tethering AR-NTD antagonists and different …

Mammalian switch/sucrose nonfermentable (mSWI/SNF) ATPase degraders have been
shown to be effective in enhancer-driven cancers by functioning to impede oncogenic …

New chemical modalities in drug discovery include molecules belonging to the bRo5
chemical space. Because of their complex and flexible structure, bRo5 compounds often …