期刊
MEDCHEMCOMM
卷 10, 期 6, 页码 1037-1041出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9md00185a
关键词
-
资金
- DFG [Kr-3886/2-1, SFB-1074, FOR2372]
- Bonn International Graduate School of Drug Sciences
- FEBS
- Slovenian Research Agency (ARRS) [P1-0208]
A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.
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