Dysregulated transcription factors (TFs) that rewire gene expression circuitry are frequently
identified as key players in disease. Although several TFs have been drugged with small …

Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and
are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer …

Challenging disease targets necessitate new approaches for therapeutic intervention.
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …

Mammalian switch/sucrose nonfermentable (mSWI/SNF) ATPase degraders have been
shown to be effective in enhancer-driven cancers by functioning to impede oncogenic …

Degrader technologies, which enable the chemical knockdown of disease-causing proteins,
are promising for drug discovery. After two decades of research, degraders using the …

Small cell lung cancer (SCLC) has limited therapeutic options and an exceptionally poor
prognosis. Understanding the oncogenic drivers of SCLC may help define novel therapeutic …

Breast cancer remains a common cause of cancer-related death in women. Therefore,
further studies are necessary for the comprehension of breast cancer and the revolution of …

Starting from a nonselective bromodomain and extraterminal (BET) inhibitor and a cereblon
ligand, we have used precise conformational control for the development of two potent and …

In the last four decades, treatment of oestrogen receptor positive (ER+) breast cancer (BCa),
has focused on targeting the estrogenic receptor signaling pathway. This signaling function …

Protein degradation is emerging as a powerful strategy to modulate protein functions and
alter cellular signaling pathways. Proteolysis-targeting chimeras (PROTACs) have been …