Cited by 300Lymphoma Diagnosis and TreatmentProtein Degradation and InhibitorsComputational Drug Discovery Methods

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A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo

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Cerchietti, Leandro C., Ghetu, Alexandru F., Zhu, Xiao, Da Silva, Gustavo F., Zhong, Shijun, Matthews, Marilyn, Bunting, Karen L., Polo, Jose M., Farès, Christophe, Arrowsmith, Cheryl H., Yang, Shao Ning, Garcia, Monica, Coop, Andrew, MacKerell, Alexander D., Privé, Gilbert G., Melnick, Ari·2010·Cancer Cell

DOI 10.1016/j.ccr.2009.12.050PMC PMC2858395

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Abstract

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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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: Cerchietti, Leandro C.
Zhu, Xiao
Zhong, Shijun
Polo, Jose M.
Farès, Christophe
Arrowsmith, Cheryl H.
Coop, Andrew
MacKerell, Alexander D.
Privé, Gilbert G.
Melnick, Ari
Venue: Cancer Cell
Publisher: Elsevier BV
Published: 2010-04
Volume: 17
Issue: 4
Pages: 400-411
ISSN: 1535-6108 (ISSN-L)
DOI: 10.1016/j.ccr.2009.12.050
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: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 1203 d)
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
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › 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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A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo

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