Department of Chemistry, Texas A & M University, Box 30012, College Station, TX 77841-3012, USA.
Chem Commun (Camb). 2019 Feb 26;55(18):2704-2707. doi: 10.1039/c9cc00163h.
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.
基于两种选择性的、已获得 FDA 批准的 CDK4/6 抑制剂，形成了 PROTACs。其中一种基于 palbociclib，能有效启动这些 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 PROTACs 在纳摩尔浓度下具有活性，似乎是 CDK4/6 的首例。
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