Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases
K Klein - RMD open, 2018 - rmdopen.bmj.com
RMD open, 2018•rmdopen.bmj.com
The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-
terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-
inflammatory properties and exhibit encouraging effects in different cell types in vitro and in
animal models resembling rheumatic diseases in vivo. Furthermore, recent studies that
focus on BRD proteins beyond BET family members are discussed.
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-
terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-
inflammatory properties and exhibit encouraging effects in different cell types in vitro and in
animal models resembling rheumatic diseases in vivo. Furthermore, recent studies that
focus on BRD proteins beyond BET family members are discussed.
The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra-terminal (BET) proteins compete for binding to acetylated histones. They have strong anti-inflammatory properties and exhibit encouraging effects in different cell types in vitro and in animal models resembling rheumatic diseases in vivo. Furthermore, recent studies that focus on BRD proteins beyond BET family members are discussed.
rmdopen.bmj.com