BET proteins, which influence gene expression and contribute to the development of cancer,
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …

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 …

BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …

Several cancer clinical trials for small molecule inhibitors of BET bromodomain proteins
have been initiated. There is enthusiasm for the anti-proliferative effect of inhibiting BRD4 …

In recent decades, the development of targeted drugs has featured prominently in the
treatment of cancer, which is among the major causes of mortality globally. Triazole-fused …

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 BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains
two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under …

Abstract The 1, 2, 4-triazolo [1, 5-a] pyrimidine (TP) heterocycle, in spite of its relatively
simple structure, has proved to be remarkably versatile as evidenced by its use in many …

Blocking the interactions between bromodomain and extraterminal (BET) proteins and
acetylated lysines of histones by small molecules has important implications for the …

Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …