The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …

With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Targeted protein degradation (TPD) is a recent strategy, utilizing the cell's proteostasis
machinery to deplete specific proteins. This represents a paradigm shift in early drug …

In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …

Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …

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), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …

Proteolysis Targeting Chimeras (PROTACs) are a rapidly expanding new therapeutic
modality inducing selective protein degradation and offering the potential of a differentiated …