Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy
Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy
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DOI：
10.1021/acschembio.6b01068
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发表时间：
2017-04-01
影响因子：
4
通讯作者：
Crews, Craig M.
中科院分区：
文献类型：
--
作者：
Ottis, Philipp;Crews, Craig M.
直到最近，唯一的办法是减少特异性。要么通过RNAi击倒靶标，要么通过抑制信号转导级联中的酶或受体来干扰信号转导。在此，我们回顾了一类新兴的小分子药物，称为PROTACs，它提供了一种新的方法来特异性靶向蛋白质及其各自的信号通路。这些异双功能分子利用内源性细胞质量控制机制，将其招募到靶蛋白上，以诱导其降解。
Until recently, the only ways' to, reduce specific. protein signaling were to either knock down the target by RNAi or to interfere with the signaling by inhibiting an enzyme or receptor within the signal transduction cascade. Herein, we review an,emerging class small Molecule pharmacological agents, called PROTACs, that present a novel approach to specifically target proteins and their respective signaling pathways. These heterobifunctional molecules utilize endogenous cellular quality control machinery by recruiting it to target proteins in order to induce their degradation.