Clinical trials for BET inhibitors run ahead of the science

G Andrieu, AC Belkina, GV Denis - Drug Discovery Today: Technologies, 2016 - Elsevier
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 …

Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases

E Kulikowski, BD Rakai… - Medicinal research …, 2021 - Wiley Online Library
Clinical development of bromodomain and extra‐terminal (BET) protein inhibitors differs
from the traditional course of drug development. These drugs are simultaneously being …

Maternal dysglycaemia, changes in the infant's epigenome modified with a diet and physical activity intervention in pregnancy: Secondary analysis of a randomised …

E Antoun, NT Kitaba, P Titcombe, KV Dalrymple… - PLoS …, 2020 - journals.plos.org
Background Higher maternal plasma glucose (PG) concentrations, even below gestational
diabetes mellitus (GDM) thresholds, are associated with adverse offspring outcomes, with …

Epigenetic drug discovery: breaking through the immune barrier

DF Tough, PP Tak, A Tarakhovsky… - Nature reviews Drug …, 2016 - nature.com
Immune-mediated diseases are clinically heterogeneous but they share genetic and
pathogenic mechanisms. These diseases may develop from the interplay of genetic factors …

Beating the odds: BETs in disease

CY Wang, P Filippakopoulos - Trends in biochemical sciences, 2015 - cell.com
Bromodomains (BRDs) are evolutionarily conserved protein interaction modules that
specifically recognise acetyl-lysine on histones and other proteins, facilitating roles in …

BET bromodomain proteins are required for glioblastoma cell proliferation

C Pastori, M Daniel, C Penas, CH Volmar… - Epigenetics, 2014 - Taylor & Francis
Epigenetic proteins have recently emerged as novel anticancer targets. Among these,
bromodomain and extra terminal domain (BET) proteins recognize lysine-acetylated …

MHC and Evolution in Teleosts

U Grimholt - Biology, 2016 - mdpi.com
Major histocompatibility complex (MHC) molecules are key players in initiating immune
responses towards invading pathogens. Both MHC class I and class II genes are present in …

BET bromodomain proteins Brd2, Brd3 and Brd4 selectively regulate metabolic pathways in the pancreatic β-cell

JT Deeney, AC Belkina, OS Shirihai, BE Corkey… - PloS one, 2016 - journals.plos.org
Displacement of B romodomain and E xtra-T erminal (BET) proteins from chromatin has
promise for cancer and inflammatory disease treatments, but roles of BET proteins in …

BRD4 regulates metastatic potential of castration-resistant prostate cancer through AHNAK

JS Shafran, GP Andrieu, B Györffy, GV Denis - Molecular Cancer Research, 2019 - AACR
The inevitable progression of advanced prostate cancer to castration resistance, and
ultimately to lethal metastatic disease, depends on primary or acquired resistance to …

BET protein inhibitor JQ1 inhibits growth and modulates WNT signaling in mesenchymal stem cells

S Alghamdi, I Khan, N Beeravolu, C McKee… - Stem Cell Research & …, 2016 - Springer
Background Efficacy and safety of anticancer drugs are traditionally studied using cancer
cell lines and animal models. The thienodiazepine class of BET inhibitors, such as JQ1, has …