Photochemical synthesis of an epigenetic focused tetrahydroquinoline library
Photochemical synthesis of an epigenetic focused tetrahydroquinoline library
复制标题
DOI：
10.1039/d1md00193k
复制
发表时间：
2021-08-25
影响因子：
4.1
通讯作者：
Burslem, George M.
中科院分区：
文献类型：
--
作者：
Green, Adam, I;Burslem, George M.
表观遗传化学探针的发现是一个重要的研究领域，有可能为多种疾病提供药物。然而，经常用于药物发现活动的商业可用文库包含的分子主要集中在狭窄的化学空间上，这主要是由于合成的简便性和先前靶向的酶类(例如，激酶)导致了表观遗传靶标的低命中率。在这里，我们描述了一个复合集合的设计和合成，它通过包含用于表观遗传靶标的特权等位基因来增强当前的筛选集合。
Discovery of epigenetic chemical probes is an important area of research with potential to deliver drugs for a multitude of diseases. However, commercially available libraries frequently used in drug discovery campaigns contain molecules that are focused on a narrow range of chemical space primarily driven by ease of synthesis and previously targeted enzyme classes (e.g., kinases) resulting in low hit rates for epigenetic targets. Here we describe the design and synthesis of a compound collection that augments current screening collections by the inclusion of privileged isosteres for epigenetic targets.