Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …

Immunometabolic intervention has been applied to treat cancer via inhibition of certain
enzymes associated with intratumoral metabolism. However, small-molecule inhibitors and …

Biomolecular condensates, membrane-less entities arising from liquid–liquid phase
separation, hold dichotomous roles in health and disease. Alongside their physiological …

The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …

Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

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

Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …

Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades
as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the …

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