Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently
degrade a target protein within cells can be a lengthy and unpredictable process, and it …

The bromodomain (BrD) is a conserved structural module found in chromatin-and
transcription-associated proteins that acts as the primary reader for acetylated lysine …

The Chematica program was used to autonomously design synthetic pathways to eight
structurally diverse targets, including seven commercially valuable bioactive substances and …

The bromodomain‐containing protein BRD9, a subunit of the human BAF (SWI/SNF)
nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer …

Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …

Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

Bromodomains are epigenetic readers of histone acetylation involved in chromatin
remodeling and transcriptional regulation. The human proteome comprises 46 …

Multi-subunit ATPase-dependent chromatin remodelling complexes SWI/SNF
(switch/sucrose non-fermentable) are fundamental epigenetic regulators of gene …