Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …

The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …

Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …

Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …

Targeted protein degradation has recently emerged as a novel option in drug discovery.
Natural protein half-life is expected to affect the efficacy of degrading agents, but to what …

Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules that co-opt the
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …

Click chemistry is universally recognized as a powerful strategy for the fast and precise
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …

Targeted protein degradation (TPD) has opened the door for drugging transcriptional
regulators, yet the number of proteins targeted and E3 ligases utilized remain limited. Here …

A principal challenge in the discovery of proteolysis targeting chimeras (PROTACs) as oral
medications is their bioavailability. To facilitate drug design, it is therefore essential to …

Regulated induced proximity targeting chimeras (RIPTACs), a new class of
heterobifunctional molecules, show promise in specifically targeting and eliminating cancer …