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

页码：1821 / 1824

页数：4

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