The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

Histone deacetylases (HDACs) are essential for maintaining homeostasis by catalyzing
histone deacetylation. Aberrant expression of HDACs is associated with various human …

Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a
targeted manner via co-opted ubiquitin ligases have enormous potential to transform the …

The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

Epigenetic changes associated with histone modifications play an important role in the
emergence and maintenance of the phenotype of various cancer types. In contrast to direct …

Bromodomain and extraterminal (BET) proteins bind acetylated lysine residues in histones
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …

Diaryl ether (DE) is a functional scaffold existing widely both in natural products (NPs) and
synthetic organic compounds. Statistically, DE is the second most popular and enduring …

An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists
of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer …

NUT carcinoma (NC) is an extremely aggressive squamous cancer with no effective therapy.
NC is driven, most commonly, by the BRD4-NUT fusion oncoprotein. BRD4-NUT combines …