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J Med Chem. 2016 Jan 28;59(2):770-4. doi: 10.1021/acs.jmedchem.5b01735. Epub 2016 Jan 8.

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

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Department of Protein Evolution, Max Planck Institute for Developmental Biology , Spemannstrasse 35, 72076 Tübingen, Germany.


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.

[Indexed for MEDLINE]

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