Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)
Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)
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DOI：
10.1039/c8cc08716d
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发表时间：
2019-01-21
影响因子：
4.9
通讯作者：
Soural, M.
中科院分区：
文献类型：
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作者：
Krajcovicova, S.;Jorda, R.;Soural, M.
由沙利度胺部分和乙烯-氧连接体组成的预装树脂可以简单快速地形成 PROTAC。通过缀合不同的蛋白激酶抑制剂说明了该程序的可行性。然后通过细胞实验证实了依鲁替尼样缀合物的生物学功能。
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.