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Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design

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/persons/resource/persons271516

Heim,  C       
Molecular Recognition and Catalysis Group, Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;
Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;

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Herrmann,  A       
Molecular Recognition and Catalysis Group, Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;
Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;

/persons/resource/persons271554

Maiwald,  S       
Molecular Recognition and Catalysis Group, Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;
Department Protein Evolution, Max Planck Institute for Biology Tübingen, Max Planck Society;

/persons/resource/persons271510

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

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Citation

Kuchta, R., Heim, C., Herrmann, A., Maiwald, S., Ng, Y., Sosič, I., et al. (2023). Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design. RSC Chemical Biology, 4(3), 229-234. doi:10.1039/D2CB00223J.


Cite as: https://hdl.handle.net/21.11116/0000-000C-8C56-6
Abstract
The Petasis borono-Mannich reaction was employed for an alternative entry towards three-branched cereblon ligands. Such compounds are capabable of making multiple interactions with the protein surface and possess a suitable linker exit vector. The high-affinity ligands were used to assemble prototypic new molecular glues and proteolysis targeting chimeras (PROTACs) targeting BRD4 for degradation. Our results highlight the importance of multicomponent reactions (MCRs) in drug discovery and add new insights into the rapidly growing field of protein degraders.