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

Authors :: Rosemary Huckvale
Alice C. Harnden
Kwai-Ming J. Cheung
Olivier A. Pierrat
Rachel Talbot
Gary M. Box
Alan T. Henley
Alexis K. de Haven Brandon
Albert E. Hallsworth
Michael D. Bright
Hafize Aysin Akpinar
Daniel S. J. Miller
Dalia Tarantino
Sharon Gowan
Angela Hayes
Emma A. Gunnell
Alfie Brennan
Owen A. Davis
Louise D. Johnson
Selby de Klerk
Craig McAndrew
Yann-Vaï Le Bihan
Mirco Meniconi
Rosemary Burke
Vladimir Kirkin
Rob L. M. van Montfort
Florence I. Raynaud
Olivia W. Rossanese
Benjamin R. Bellenie
Swen Hoelder
Source :: Journal of Medicinal Chemistry. 65:8191-8207
Publication Year :: 2022
Publisher :: American Chemical Society (ACS), 2022.
Abstract: 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

Subjects :: Gene Expression Regulation, Neoplastic
Mice
Carcinogenesis
Drug Discovery
Proto-Oncogene Proteins c-bcl-6
Animals
Humans
Molecular Medicine

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