期刊
CHEMMEDCHEM
卷 14, 期 4, 页码 362-385出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800738
关键词
acetylated lysines; chemical probes; epigenetics; non-BET bromodomains; target validation
资金
- GlaxoSmithKline R&D (Stevenage, UK)
- EPSRC [EP/S035990/1, EP/I037229/1] Funding Source: UKRI
The bromodomain and extra terminal (BET) family of bromodomain-containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high-quality chemical probes for their tandem bromodomains. In turn, these chemical probes have helped reveal the profound biological role of the BET bromodomains and their role in disease, ultimately leading to a number of molecules in active clinical development. However, the BET subfamily represents just 8/61 of the known human bromodomains, and attention has now expanded to the biological role of the remaining 53 non-BET bromodomains. Rapid growth of this research area has been accompanied by a greater understanding of the requirements for an effective bromodomain chemical probe and has led to a number of new non-BET bromodomain chemical probes being developed. Advances since December 2015 are discussed, highlighting the strengths/caveats of each molecule, and the value they add toward validating the non-BET bromodomains as tractable therapeutic targets.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据