A 110-amino acid protein domain which recognises acetylated lysine residues on the N-terminal tails of histone. It is present in over 100 proteins, especially chromatin-associated proteins—e.g., gnc5, peregrin, Snf2, tafii-250.
The trial will evaluate the combination, safety and efficacy of the Company's ZEN-3694, a novel and differentiated bromodomain and extra-terminal domain inhibitor, and Pfizer's talazoparib, a poly ADP ribose polymerase inhibitor, in patients with locally advanced or metastatic triple negative breast cancer without germline BRCA1/2 mutations.
has signed an exclusive global license agreement that provides OHM Oncology with the rights for the development, manufacture and commercialization of APL-581, as well as related molecules from Aptose's dual bromodomain and extra-terminal domain motif (BET) protein and kinase inhibitor program.
Microarray experiments conducted on leukemia cell lines treated with the bromodomain inhibitor JQ1 showed that JQ1 causes a significant downregulation of S100A8 and S100A9 transcripts in OCI-AML3 cells (Figure 1).
demonstrated that the inhibition of bromodomain protein BRD4 could alleviate the expression of oncogenic lncRNA HOTAIR in GBM patients, exerting an antiproliferation effect by inducing cell cycle arrest in GBM cells [160, 161].
DNMT inhibitors (DNMTi), histone deacetylase inhibitors (HDACi), and inhibitors of the bromodomain and extraterminal motif proteins (iBET), approved by the US Food and Drug Administration (FDA), are actually in clinical trials for several malignancies and they are reviewed in detail in .