A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo
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The BCL6 transcriptional repressor is the most frequently involved oncogene in diffuse large B cell lymphoma (DLBCL). We combined computer-aided drug design with functional assays to identify low-molecular-weight compounds that bind to the corepressor binding groove of the BCL6 BTB domain. One such compound disrupted BCL6/corepressor complexes in vitro and in vivo, and was observed by X-ray crystallography and NMR to bind the critical site within the BTB groove. This compound could induce expression of BCL6 target genes and kill BCL6-positive DLBCL cell lines. In xenotransplantation experiments, the compound was nontoxic and potently suppressed DLBCL tumors in vivo. The compound also killed primary DLBCLs from human patients.
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Several peptide and small molecule inhibitors targeting BCL6 have shown efficacy in vivo, but only at high concentrations, which has limited their translation into clinical therapeutic agents.
“Several peptide and small molecule inhibitors targeting BCL6 have shown efficacy in vivo, but only at high concentrations, which has limited their translation into clinical therapeutic agents13,14.”
From Small-molecule-induced polymerization triggers degradation of BCL6 (2020) · cites this paper as [13]
BCL6 is a promising drug target for non-Hodgkin lymphomas including diffuse large B cell lymphoma and follicular lymphoma.
“BCL6 is a promising drug target for non-Hodgkin lymphomas including diffuse large B cell lymphoma (DLBCL)13,14 and follicular lymphoma15.”
From Small-molecule-induced polymerization triggers degradation of BCL6 (2020) · cites this paper as [13]
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- Authors
- Cerchietti, L. C., Ghetu, A. F., Zhu, X., Da Silva, G. F., Zhong, S., Matthews, M., Bunting, K. L., Polo, J. M., Farès, C., Arrowsmith, C. H., Yang, S. N., Garcia, M., Coop, A., MacKerell, A. D., Privé, G. G., & Melnick, A.
- Affiliations
- Cornell University (US)
- University of Maryland, Baltimore (US)
- Albert Einstein College of Medicine (US)
- University of Toronto (CA)
- Corresponding author
- MacKerell, Alexander D.
- Privé, Gilbert G.
- Melnick, Ari
- ORCID
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2010-04
- Volume
- 17
- Issue
- 4
- Pages
- 400-411
- ISSN
- 1535-6108 (ISSN-L)
- PMC
- PMC2858395
- OpenAlex
- W2018796139
- Cited by
- 288
- References
- 53
- Citations by year
- 2026: 4 · 2025: 13 · 2024: 9 · 2023: 9 · 2022: 13 · 2021: 12 · 2020: 20 · 2019: 19 · 2018: 16 · 2017: 15 · 2016: 30 · 2015: 28 · 2014: 24 · 2013: 28 · 2012: 22
- FWCI
- 16.50
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Cancer Cell (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Max Planck Digital Library (submittedVersion)
- MPG.PuRe (Max Planck Society) (submittedVersion, cc-by)
- Funders
- Canadian Cancer Society
- Leukemia and Lymphoma Society
- National Cancer Institute (R01 CA104348)
- National Institutes of Health (HL082670, CA107331, CA120215)
- University of Maryland Foundation Inc.
- Chemotherapy Foundation
- Samuel Waxman Cancer Research Foundation
- Topics
- Health Sciences › Medicine › Pathology and Forensic Medicine › Lymphoma Diagnosis and Treatment
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Keywords
- BCL6, diffuse large B-cell lymphoma, small molecule inhibitors, BTB domain, transcriptional repressor, computer-aided drug design, xenotransplantation, oncogenes
- MeSH terms
- Animals, Cell Division, Cell Survival, Humans, Mice, Inbred C57BL, Models, Molecular, Protein Conformation, Proto-Oncogene Proteins, Repressor Proteins, Transcription, Genetic, Zinc Fingers, Lymphoma, Large B-Cell, Diffuse, Crystallography, X-Ray, Mice
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