Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

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 …

During the past 10 years, preclinical studies implicating sustained androgen receptor (AR)
signalling as the primary driver of castration-resistant prostate cancer (CRPC) have led to …

In 2011, AstraZeneca embarked on a major revision of its research and development (R&D)
strategy with the aim of improving R&D productivity, which was below industry averages in …

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 …

Most prostate cancers are androgen-sensitive malignancies whose growths depend on the
transcriptional activity of the androgen receptor (AR). In the 1940s, Charles Huggins …

Prostate and breast cancer are the two cancers with the highest incidence in men and
women, respectively. Here, we focus on the known biology of acquired resistance to …

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 …

The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …

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