基于沙利度胺的蛋白水解靶向嵌合体（PROTAC）的固相合成。
Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC).
机构信息
Department of Organic Chemistry, Faculty of Science, Palacky University, 17. listopadu 12, 771 46 Olomouc, Czech Republic.
出版信息
Chem Commun (Camb). 2019 Jan 17;55(7):929-932. doi: 10.1039/c8cc08716d.
PMID:30601480
Abstract
A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.
摘要
一种预装载的树脂，由沙利度胺部分和乙烯氧基连接子组成，允许简单快速地形成 PROTAC。该方法的可行性通过连接不同的蛋白激酶抑制剂得到了证明。然后通过细胞实验证实了一种类似伊布替尼的缀合物的生物学功能。
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