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Habib Bouguenina; Scarpino, Andrea; O'Hanlon, Jack A; Warne, Justin; Wang, Hannah Z; Laura Chan Wah Hak; Sadok, Amine; McAndrew, P Craig; Stubbs, Mark; Pierrat, Olivier A; Hahner, Tamas; Cabry, Marc P; Yann‐Vaï Le Bihan; Mitsopoulos, Costas; Sialana, Fernando J; Roumeliotis, Theodoros I; Burke, Rosemary; Rob L M van Montfort; Choudhari, Jyoti; Chopra, Rajesh; Caldwell, John J; Collins, Ian
Chembiochem : a European journal of chemical biology, 12/2023, Letnik: 24, Številka: 23Journal Article
E3 ligase mediated targeted protein degradation is an ever more important area in drug discovery. In the case of cereblon two avenues exist; either heterobifunctional PROTACs, or discrete cereblon ligands that induce a specific neosubstrate degron association to the complex. Here we present a degron blocking approach, whereby structural and in silico understandings of degron association has directed ligand design to block IMiD‐like binding of degron containing neosubstrates, thus enhancing PROTAC selectivity. More information can be found in the Research Article by H. Bouguenina, J. J. Caldwell et al.
