PROTAC-mediated crosstalk between E3 ligases

被引：67
|
作者：
Steinebach, Christian [1 ]
Kehm, Hannes [2 ]
Lindner, Stefanie [2 ]
Lan Phuong Vu [1 ]
Koepff, Simon [2 ]
Marmol, Alvaro Lopez [3 ]
Weiler, Corinna [1 ]
Wagner, Karl G. [3 ]
Reichenzeller, Michaela [2 ]
Kroenke, Jan [2 ]
Guetschow, Michael [1 ,4 ]
机构：
[1] Univ Bonn, Pharmaceut Chem 1, Pharmaceut Inst, Immenburg 4, D-53121 Bonn, Germany
[2] Univ Hosp Ulm, Dept Internal Med 3, Albert Einstein Allee 23, D-89081 Ulm, Germany
[3] Univ Bonn, Pharmaceut Technol, Pharmaceut Inst, Gerhard Domagk Str 3, D-53121 Bonn, Germany
[4] DKFZ, Mol Genet, Neuenheimer Feld 260, D-69120 Heidelberg, Germany
来源：
CHEMICAL COMMUNICATIONS | 2019年 / 55卷 / 12期
关键词：
UBIQUITIN LIGASE; PROTEIN-DEGRADATION; SMALL-MOLECULE; LENALIDOMIDE; CEREBLON; TARGET; IDENTIFICATION; OPTIMIZATION; MODULATION;
D O I：
10.1039/c8cc09541h
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
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.
引用
收藏
页码：1821 / 1824
页数：4
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