Abstract Bromodomain-containing protein 4 (BRD4) has been identified as a potential target
in the treatment of many cancers and several BRD4 inhibitors have entered clinical studies …

Targeted protein degradation (TPD) holds immense promise for drug discovery, but
mechanisms of acquired resistance to degraders remain to be fully identified. Here, we used …

Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

Targeted protein degradation (TPD) holds great promise for biological inquiry and
therapeutic development. However, it still remains elusive to destruct DNA/RNA binding …

The anticancer agent indisulam inhibits cell proliferation by causing degradation of RBM39,
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …

BRD4, a bromodomain and extraterminal domain (BET) family member, is an attractive
target in multiple pathological settings, particularly cancer. While BRD4 inhibitors have …

Inducing macromolecular interactions with small molecules to activate cellular signaling is a
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …

The biological role played by non-BET bromodomains remains poorly understood, and it is
therefore imperative to identify potent and highly selective inhibitors to effectively explore the …

Molecular glue (MG) degraders are monovalent small molecule compounds that co-opt E3
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …