PROTAC 介导的 E3 连接酶串扰。
PROTAC-mediated crosstalk between E3 ligases.
机构信息
Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
出版信息
Chem Commun (Camb). 2019 Feb 5;55(12):1821-1824. doi: 10.1039/c8cc09541h.
PMID:30672516
Abstract
Small-molecule heterobifunctional degraders can effectively control protein levels and are useful research tools. We assembled proteolysis targeting chimeras (PROTACs) from a cereblon (CRBN) and a von-Hippel-Lindau (VHL) ligase ligand and demonstrated a PROTAC-induced heterodimerization of the two E3 ligases leading to unidirectional and efficient degradation of CRBN.
摘要
小分子杂双功能降解剂可以有效地控制蛋白质水平，是非常有用的研究工具。我们从 cereblon (CRBN) 和 von-Hippel-Lindau (VHL) 连接酶配体组装了蛋白水解靶向嵌合体 (PROTACs)，并证明了 PROTAC 诱导的两种 E3 连接酶的杂二聚化导致 CRBN 的单向和有效降解。
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