The development of effective pharmacological inhibitors of multidomain scaffold proteins,
notably transcription factors, is a particularly challenging problem. In part, this is because many …

Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts
have been limited to chromatin modifying enzymes, or so-called epigenetic ‘writers’ and ‘…

Epigenetic pathways can regulate gene expression by controlling and interpreting chromatin
modifications. Cancer cells are characterized by altered epigenetic landscapes, and …

Chromatin modifications, especially histone-tail acetylation, have been implicated in memory
formation. Increased histone-tail acetylation induced by inhibitors of histone deacetylases (…

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are
effective treatments for a subset of non–small cell lung cancers. In particular, cancers with …

Direct inhibition of transcription factor complexes remains a central challenge in the discipline
of ligand discovery. In general, these proteins lack surface involutions suitable for high-…

There is considerable evidence that chromosome structure plays important roles in gene
control, but we have limited understanding of the proteins that contribute to structural …

We have shown that the proteasome inhibitor bortezomib (formerly known as PS-341)
triggers significant antitumor activity in multiple myeloma (MM) in both preclinical models and …

Bromodomain inhibition comprises a promising therapeutic strategy in cancer, particularly
for hematologic malignancies. To date, however, genomic biomarkers to direct clinical …

Chromosomal rearrangements without gene fusions have been implicated in leukemogenesis
by causing deregulation of proto-oncogenes via relocation of cryptic regulatory DNA …