PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer
PROTACs suppression of CDK4/6, crucial kinases for cell cycle regulation in cancer
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DOI：
10.1039/c9cc00163h
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发表时间：
2019-03-04
影响因子：
4.9
通讯作者：
Burgess, Kevin
中科院分区：
文献类型：
--
作者：
Zhao, Bosheng;Burgess, Kevin
形成了基于两种选择性FDA批准的CDK 4/6抑制剂的PROTAC。其中一种基于palbociclib，可有效启动这些CDK蛋白的降解，并抑制视网膜母细胞瘤蛋白（Rb）的磷酸化，导致细胞周期停滞。这些PROTAC在纳摩尔浓度下具有活性，并且似乎是CDK 4/6的第一个。
PROTACs based on two selective, FDA approved, CDK4/6 inhibitors were formed. One of them, based on palbociclib, potently initiates degradation of these CDK proteins, and suppresses phosphorylation of retinoblastoma protein (Rb) leading to cell cycle arrest. These PROTACs are active at nanomolar concentrations, and appear to be the first for CDK4/6.