Achieving <i>In Vivo</i> Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders
Benjamin R. Bellenie, Kwai-Ming J. Cheung, Ana Varela, Olivier A. Pierrat, Gavin W. Collie, Gary Box, Michael D. Bright, Sharon Gowan, Angela Hayes, Matthew J. Rodrigues, Kartika N. Shetty, Michael Carter, Owen A. Davis, Alan T. Henley, Paolo Innocenti, Louise D. Johnson, Manjuan Liu, Selby de Klerk, Yann‐Vaï Le Bihan, Matthew G. Lloyd, Craig McAndrew, Erald Shehu, Rachel Talbot, Hannah L. Woodward, Rosemary Burke, Vladimir Kirkin, Rob L. M. van Montfort, Florence I. Raynaud, Olivia W. Rossanese, Swen Hoelder
Abstract
]imidazol-2-one (CCT369260), which reduces BCL6 levels in a lymphoma xenograft mouse model following oral dosing.
Topics & Concepts
BCL6ChemistryIn vivoGerminal centerRepressorLymphomaCancer researchBiochemistryB cellTranscription factorBiologyGeneticsGeneImmunologyAntibodyProtein Degradation and InhibitorsCAR-T cell therapy researchUbiquitin and proteasome pathways