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

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.

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Item Permalink: https://hdl.handle.net/21.11116/0000-000A-926E-6 Version Permalink: https://hdl.handle.net/21.11116/0000-000B-B2CE-4

Genre: Journal Article

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Creators:
Boichenko, I^{1, 2}, Author
Deiss, S^{1, 2}, Author
Bär, K¹, Author
Hartmann, MD^{1, 3}, Author
Hernandez Alvarez, B^{1, 2}, Author

Affiliations:
1Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society, ou_3375791
2Conservation of Protein Structure and Function Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society, ou_3477389
3Molecular Recognition and Catalysis Group, Department Protein Evolution, Max Planck Institute for Developmental Biology, Max Planck Society, ou_3477392

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Abstract: 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.

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Dates: Date issued: 2016-01

Publication Status: Issued

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Identifiers: DOI: 10.1021/acs.jmedchem.5b01735
PMID: 26730808

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Title: Journal of Medicinal Chemistry

Source Genre: Journal

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Publ. Info: Washington DC : ACS Publications

Pages: - Volume / Issue: 59 (2) Sequence Number: - Start / End Page: 770 - 774 Identifier: ISSN: 0022-2623
CoNE: https://pure.mpg.de/cone/journals/resource/110992357271168