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TitleDiscovery of Potent and Selective BCL6 Ligand-Directed Degrader (LDD), BCL6-760.
Journal, issue, pagesJ Med Chem, Vol. 68, Issue 20, Page 21502-21519, Year 2025
Publish dateOct 23, 2025
AuthorsHunter P Shunatona / Natalie Holmberg Douglas / Jayce Rhodes / William Thomas / Diogo Da Silva / Jim Gamez / Matt Groza / Andy Christoforou / Jinyi Zhu / Scott Johnson / Dharmpal Dodd / Dehua Huang / Jennifer Griffin / Giulianna Miseo / Brandon Whitefield / Dahlia Weiss / James Rader / Elif Kuzu / Jim Leisten / Joselyn Del Rosario / Lihong Shi / Mary Matyskiela / Philip P Chamberlain / Peter Belmont / Matt Alexander / Christoph W Zapf / Lynda Groocock / Deborah S Mortensen /
PubMed AbstractThe discovery of a potent and selective BCL6 ligand-directed degrader (LDD), BCL6-760 () is described. Through structure-activity relationships, the most potent heterobifunctional degraders of BCL6 ...The discovery of a potent and selective BCL6 ligand-directed degrader (LDD), BCL6-760 () is described. Through structure-activity relationships, the most potent heterobifunctional degraders of BCL6 were found to be those containing short aminopiperidine linkers in combination with an indazole-based cereblon (CRBN)-binding moiety (CBM). In vitro ADME profiling of potent molecules identified BCL6-760 as an ideal molecule for use in in vivo experiments due to its good passive permeability, solubility, and microsomal stability. Mechanistic studies confirmed that BCL6 degradation is CRBN mediated, and proteomic assessment indicates a clean and selective degradation profile. BCL6-760 exhibited good oral mouse PK and was capable of penetrant and sustained PD effects. At 60 mg/kg BID dosing, BCL6-760 achieves >90% BCL6 reduction and leads to an overall 64% tumor volume reduction in an OCI-LY-1 mouse xenograft efficacy model.
External linksJ Med Chem / PubMed:41055242
MethodsEM (single particle)
Resolution3.15 Å
Structure data

72086

9q03

EMDB-72086, PDB-9q03:
Cryo-EM structure of ternary complex BCL6-CRBN-DDB1 with BCL6-760 (LDD, local refined)
Method: EM (single particle) / Resolution: 3.15 Å

Chemicals

ChemComp-ZN:
Unknown entry

PDB-1cm7:
3-ISOPROPYLMALATE DEHYDROGENASE FROM ESCHERICHIA COLI

Source
  • homo sapiens (human)
KeywordsLIGASE / Cereblon / BCL6 / LDD / degrader / E3

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