Small-molecule drug discovery has traditionally focused on occupancy of a binding site that
directly affects protein function, and this approach typically precludes targeting proteins that …

Traditional pharmaceutical drug discovery is almost exclusively focused on directly
controlling protein activity to cure diseases. Modulators of protein activity, especially …

Control of protein levels by nucleic-acid-based technologies has proven to be a useful
research tool but lacks the advantages of small molecules with respect to cell permeability …

The cancer genomics revolution has served up a plethora of promising and challenging
targets for the drug discovery community. The field of targeted protein degradation (TPD) …

Importance The androgen receptor (AR) pathway is emerging as a potential therapeutic
target in breast cancer. To date, AR-targeted drugs have been approved only for treatment of …

Nuclear receptors (NRs) are transcription factors actively involved in many aspects of human
physiology and pathology, serving as sensors of stimuli, master regulators of downstream …

Simple Summary The CREB-binding protein (CBP) and p300 are paralogous lysine
acetyltransferases that serve as critical co-activators for transcription factors involved in …

Bromodomain-containing protein 4 (Brd4) plays an important role in mediating the
expression of genes involved in cancers and non-cancer diseases such as inflammatory …

The discovery of androgen dependence in prostate cancer in 1941 by Huggins and
colleagues has remained the backbone for the treatment of this disease. However, although …

Protein homeostasis networks are highly regulated systems responsible for maintaining the
health and productivity of cells. Whereas therapeutics have been developed to disrupt …