Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

[Image: see text] Deregulation of the transcriptional repressor BCL6 enables tumorigenesis of germinal center B-cells, and hence BCL6 has been proposed as a therapeutic target for the treatment of diffuse large B-cell lymphoma (DLBCL). Herein we report the discovery of a series of benzimidazolone in...

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Autores principales: Bellenie, Benjamin R., Cheung, Kwai-Ming J., Varela, Ana, Pierrat, Olivier A., Collie, Gavin W., Box, Gary M., Bright, Michael D., Gowan, Sharon, Hayes, Angela, Rodrigues, Matthew J., Shetty, Kartika N., Carter, Michael, Davis, Owen A., Henley, Alan T., Innocenti, Paolo, Johnson, Louise D., Liu, Manjuan, de Klerk, Selby, Le Bihan, Yann-Vaï, Lloyd, Matthew G., McAndrew, P. Craig, Shehu, Erald, Talbot, Rachel, Woodward, Hannah L., Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Hoelder, Swen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7184563/
https://www.ncbi.nlm.nih.gov/pubmed/32275432
http://dx.doi.org/10.1021/acs.jmedchem.9b02076

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