作者
Guillaume Andrieu, Anna C Belkina, Gerald V Denis
发表日期
2016/3/1
来源
Drug Discovery Today: Technologies
卷号
19
页码范围
45-50
出版商
Elsevier
简介
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, one of the targets of these inhibitors, which is thought to cooperate with MYC, a long-desired target for cancer therapeutics. However, no current inhibitor is selective for BRD4 among the three somatic BET proteins, which include BRD2 and BRD3; their respective functions are partially overlapping and none are functionally redundant with BRD4. Each BET protein controls distinct transcriptional pathways that are important for functions beyond cancer cell proliferation, including insulin production, cytokine gene transcription, T cell differentiation, adipogenesis and most seriously, active repression of dangerous latent viruses like HIV. BET inhibitors have been shown to reactivate HIV in human cells. Failure to appreciate that at concentrations …
引用总数
20162017201820192020202120222023202412037535241222313
学术搜索中的文章
G Andrieu, AC Belkina, GV Denis - Drug Discovery Today: Technologies, 2016