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  • Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design [Elektronski vir]
    Kuchta, Robert ...
    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.
    Source: RSC chemical biology. - ISSN 2633-0679 (Vol. 4, iss. 3, 2023, str. 229-234)
    Type of material - e-article ; adult, serious
    Publish date - 2023
    Language - english
    COBISS.SI-ID - 136507395

    Link(s):

    https://pubs.rsc.org/en/content/articlelanding/2023/cb/d2cb00223j
    Repository of the University of Ljubljana – RUL
    DOI

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