Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …

Protein–protein interactions (PPI) were once considered 'undruggable', but clinical
successes, driven by advanced methods in drug discovery, have challenged that notion …

CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors,
represents an attractive target for various diseases, including malignant tumor. The …

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

Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …

Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially
interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical …

Privileged scaffolds as starting points toward biologically active molecules represent a
neuralgic point in drug discovery. The ability of synthetic chemists concerned with their …

CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential
target for prostate cancer treatment. Herein, we report the structural optimization of a series …

An electrochemical intramolecular oxytrifluoromethylation of N-tethered alkenyl alcohols
was developed providing straightforward access to CF3-containing morpholines derivatives …

Bromodomain-containing proteins include bromodomain and extra-terminal (BET) and non-
BET families. Due to the conserved bromodomain (BD) module between BD-containing …