A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands

被引：20

作者：

Boichenko, Iuliia ^{[1
]}

Deiss, Silvia ^{[1
]}

Baer, Kerstin ^{[1
]}

Hartmann, Marcus D. ^{[1
]}

Alvarez, Birte Hernandez ^{[1
]}

机构：

[1] Max Planck Inst Dev Biol, Dept Prot Evolut, Spemannstr 35, D-72076 Tubingen, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 59卷 / 02期

关键词：

E3 UBIQUITIN LIGASE; LENALIDOMIDE; THALIDOMIDE; DEGRADATION; TARGET; COMPLEX; POMALIDOMIDE; MIMICS; IKAROS; CELLS;

D O I：

10.1021/acs.jmedchem.5b01735

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cereblon serves as an ubiquitin ligase substrate receptor that can be tuned toward different target proteins by various cereblon-binding agents. This offers one of the most promising avenues for targeted protein degradation in cancer therapy, but cereblon binding can also mediate teratogenic effects. We present an effective assay that is suited for high throughput screening of compound libraries for off-target cereblon interactions but also can guide lead optimization and rational design of novel cereblon effector molecules.

引用

页码：770 / 774

页数：5

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