Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

[Image: see text] To identify new chemical series with enhanced binding affinity to the BTB domain of B-cell lymphoma 6 protein, we targeted a subpocket adjacent to Val18. With no opportunities for strong polar interactions, we focused on attaining close shape complementarity by ring fusion onto our...

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Detalles Bibliográficos
Autores principales: Davis, Owen A., Cheung, Kwai-Ming J., Brennan, Alfie, Lloyd, Matthew G., Rodrigues, Matthew J., Pierrat, Olivier A., Collie, Gavin W., Le Bihan, Yann-Vaï, Huckvale, Rosemary, Harnden, Alice C., Varela, Ana, Bright, Michael D., Eve, Paul, Hayes, Angela, Henley, Alan T., Carter, Michael D., McAndrew, P. Craig, Talbot, Rachel, Burke, Rosemary, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Meniconi, Mirco, 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/PMC9234963/
https://www.ncbi.nlm.nih.gov/pubmed/35657291
http://dx.doi.org/10.1021/acs.jmedchem.1c02174

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