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 …

Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …

Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …

Inhibition of PCAF bromodomain has been validated as a promising strategy for the
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …

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

With the bromodomain (BRD) inhibitor JQ1, a remarkable success story of BRD4 as a novel
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …

General control non-depressible 5 (GCN5) or lysine acetyltransferase 2A (KAT2A) is one of
the most highly studied histone acetyltransferases. It acts as both histone acetyltransferase …

Targeting PCAF with small inhibitor molecules has emerged as a potential therapeutic
strategy for the treatment of cancer. Recently, L-45 was identified as a potent …

In recent years, substantial research has been conducted on molecular mechanisms and
inhibitors targeting bromodomains (BRDs) and extra-terminal (BET) family proteins. On this …