Discovery of Potent and Selective BCL6 Ligand-Directed Degrader (LDD), BCL6-760

The discovery of a potent and selective BCL6 ligand-directed degrader (LDD), BCL6-760 (<b>45</b>) is described. Through structure–activity relationships, the most potent heterobifunctional degraders of BCL6 were found to be those containing short aminopiperidine linkers in combination wi...

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1. Verfasser:	Hunter P. Shunatona (6899231) (author)
Weitere Verfasser:	Natalie Holmberg Douglas (22384822) (author), Jayce Rhodes (16521098) (author), William Thomas (2538196) (author), Diogo Da Silva (11021745) (author), Jim Gamez (22384825) (author), Matt Groza (22384828) (author), Andy Christoforou (1784647) (author), Jinyi Zhu (5696405) (author), Scott Johnson (150270) (author), Dharmpal Dodd (11458613) (author), Dehua Huang (2708470) (author), Jennifer Griffin (4386358) (author), Giulianna Miseo (22384831) (author), Brandon Whitefield (1562377) (author), Dahlia Weiss (22384834) (author), James Rader (22384837) (author), Elif Kuzu (22384840) (author), Jim Leisten (1562386) (author), Joselyn Del Rosario (14985411) (author), Lihong Shi (481066) (author), Mary Matyskiela (22384843) (author), Philip P. Chamberlain (2422576) (author), Peter Belmont (22384846) (author), Matt Alexander (8596557) (author), Christoph W. Zapf (2019895) (author), Lynda Groocock (18218650) (author), Deborah S. Mortensen (1562317) (author)
Veröffentlicht:	2025
Schlagworte:	Biophysics Biochemistry Cell Biology Genetics Molecular Biology Pharmacology Biotechnology Cancer Science Policy Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified vivo experiments due vitro adme profiling sustained pd effects proteomic assessment indicates mechanistic studies confirmed kg bid dosing good passive permeability tumor volume reduction selective degradation profile selective bcl6 ligand ldd ), bcl6 potent heterobifunctional degraders 760 (< b bcl6 reduction bcl6 degradation overall 64 microsomal stability ideal molecule directed degrader crbn mediated cbm ). based cereblon 760 achieves 60 mg
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Discovery of Potent and Selective BCL6 Ligand-Directed Degrader (LDD), BCL6-760

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