Targeted protein degradation (TPD) is a promising strategy to remove deleterious proteins
for therapeutic benefit and to probe biological pathways. The past two decades have …

Targeted protein degradation has generated excitement in chemical biology and drug
discovery throughout academia and industry. By hijacking the machinery responsible for …

Targeted protein degradation is a powerful strategy to address the canonically undruggable
proteome. However, current technologies are limited to targets with cytosolically-accessible …

Classic small molecule inhibitors that directly target pathogenic proteins typically rely on the
accessible binding sites to achieve prolonged occupancy and influence protein functions …

In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …

Membrane proteins are a crucial class of therapeutic targets that remain challenging to
modulate using traditional occupancy-driven inhibition strategies or current proteolysis …

In the scope of targeted protein degradation (TPD), proteolysis-targeting chimeras
(PROTACs), leveraging the ubiquitin–proteasome system, have been extensively studied …

Highlights•Targeted-protein degradation supports fundamental discovery and drug
development.•Biologics-based degraders target intracellular, extracellular, and membrane …

Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This
typically relies on a measurable biochemical readout and accessible binding sites whose …

Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …