Electrophilic biocompatible warheads, particularly cysteine-reactive acrylamides, have
enabled the development of covalent inhibitor drugs and chemical biology probes, but …

Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …

The ubiquitin-proteasome system (UPS) is the major machinery mediating specific protein
turnover in eukaryotic cells. By ubiquitylating unwanted, damaged, or harmful proteins and …

Degraders have illustrated that compound‐induced proximity to E3 ubiquitin ligases can
prompt the ubiquitination and degradation of disease‐relevant proteins. Hence, this …

Molecular glues are a class of small molecules that stabilize the interactions between
proteins. Naturally occurring molecular glues are present in many areas of biology where …

Acute myeloid leukemia (AML) is a hematologic malignancy for which several epigenetic
regulators have been identified as therapeutic targets. Here we report the development of …

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …

Cereblon (CRBN) is a ubiquitin ligase (E3) substrate receptor protein co-opted by CRBN E3
ligase modulatory drug (CELMoD) agents that target therapeutically relevant proteins for …

Thalidomide and its derivatives are molecular glues that bind cereblon (CRBN), a
component of an E3 ubiquitin ligase complex, and mediate protein interactions with …

Proteolysis-targeting chimeras (PROTACs) are molecules that induce proximity between
target proteins and E3 ligases triggering target protein degradation. Pomalidomide, a widely …