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

Boichenko, I; Deiss, S; Bär, K; Hartmann, MD; Hernandez Alvarez, B

doi:10.1021/acs.jmedchem.5b01735

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

MPG-Autoren

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Boichenko, I
Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;
Conservation of Protein Structure and Function Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;

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Deiss, S
Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;
Conservation of Protein Structure and Function Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;

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Bär, K
Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;

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Hartmann, MD
Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;
Molecular Recognition and Catalysis Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;

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Hernandez Alvarez, B
Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;
Conservation of Protein Structure and Function Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society;

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Zitation

Boichenko, I., Deiss, S., Bär, K., Hartmann, M., & Hernandez Alvarez, B. (2016). A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands. Journal of Medicinal Chemistry, 59(2), 770-774. doi:10.1021/acs.jmedchem.5b01735.

Zitierlink: https://hdl.handle.net/21.11116/0000-000A-926E-6

Zusammenfassung

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.