溴尿嘧啶
BRD4
药物发现
药品
医学
临床试验
药物开发
药理学
候选药物
计算生物学
生物信息学
生物
内科学
表观遗传学
遗传学
基因
作者
Mehrosh Pervaiz,Pankaj Mishra,Stefan Günther
标识
DOI:10.1002/tcr.201800074
摘要
Abstract 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 trials. But not all of the great prospects of BRDs as drug targets may become true. First evaluations of ongoing clinical trials revealed that treatment with BET‐inhibitors can be accompanied with significant toxic side effects and the validation of the therapeutic benefit of BET‐inhibitors compared to existing therapies is still pending. New strategies that may overcome possible obstacles in BRD drug discovery include combination therapies with other agents, dual target inhibitors, and proteolysis targeting chimeras (PROTACs). Furthermore, non‐BET proteins seem promising drug targets as well. Most recently, BRDs have been identified as putative targets to treat parasitic diseases such as malaria. Milestones in BRD drug discovery are reviewed and promising new developments are evaluated.
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