20.500.12556/RUL-144171 Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design 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. the Petasis borono-Mannich reaction Strecker synthesis CRBN ligands true false true Angleški jezik Angleški jezik Članek v reviji 2023-02-02 11:30:56 2023-02-02 11:30:58 2023-02-04 03:18:39 0000-00-00 00:00:00 2023 0 0 iss. Vol. 2023 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 2023-01-01 615.4:54 2633-0679 10.1039/D2CB00223J 136507395 Fakulteta za farmacijo 0 0 0