Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

[Image: see text] The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degrader CCT369260 to CCT373566, a highly potent probe suitable for sustaine...

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Detalles Bibliográficos
Autores principales: Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9234961/
https://www.ncbi.nlm.nih.gov/pubmed/35653645
http://dx.doi.org/10.1021/acs.jmedchem.1c02175

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9234961/
https://www.ncbi.nlm.nih.gov/pubmed/35653645
http://dx.doi.org/10.1021/acs.jmedchem.1c02175

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