Cited by 188Lymphoma Diagnosis and TreatmentComputational Drug Discovery MethodsChronic Lymphocytic Leukemia Research

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Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma

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Cardenas, Mariano G., Yu, Wenbo, Beguelin, Wendy, Teater, Matthew R., Geng, Huimin, Goldstein, Rebecca L., Oswald, Erin, Hatzi, Katerina, Yang, Shao-Ning, Cohen, Joanna, Shaknovich, Rita, Vanommeslaeghe, Kenno, Cheng, Huimin, Liang, Dongdong, Cho, Hyo Je, Abbott, Joshua, Tam, Wayne, Du, Wei, Leonard, John P., Elemento, Olivier, Cerchietti, Leandro, Cierpicki, Tomasz, Xue, Fengtian, MacKerell, Alexander D., Melnick, Ari M.·2016·Journal of Clinical Investigation

DOI 10.1172/jci85795PMC PMC5004937

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Abstract

Diffuse large B cell lymphomas (DLBCLs) arise from proliferating B cells transiting different stages of the germinal center reaction. In activated B cell DLBCLs (ABC-DLBCLs), a class of DLBCLs that respond poorly to current therapies, chromosomal translocations and amplification lead to constitutive expression of the B cell lymphoma 6 (BCL6) oncogene. The role of BCL6 in maintaining these lymphomas has not been investigated. Here, we designed small-molecule inhibitors that display higher affinity for BCL6 than its endogenous corepressor ligands to evaluate their therapeutic efficacy for targeting ABC-DLBCL. We used an in silico drug design functional-group mapping approach called SILCS to create a specific BCL6 inhibitor called FX1 that has 10-fold greater potency than endogenous corepressors and binds an essential region of the BCL6 lateral groove. FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. Low doses of FX1 induced regression of established tumors in mice bearing DLBCL xenografts. Furthermore, FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo. These findings indicate that ABC-DLBCL is a BCL6-dependent disease that can be targeted by rationally designed inhibitors that exceed the binding affinity of natural BCL6 ligands.

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Authors: Cardenas, M. G., Yu, W., Beguelin, W., Teater, M. R., Geng, H., Goldstein, R. L., Oswald, E., Hatzi, K., Yang, S.-N., Cohen, J., Shaknovich, R., Vanommeslaeghe, K., Cheng, H., Liang, D., Cho, H. J., Abbott, J., Tam, W., Du, W., Leonard, J. P., Elemento, O., Cerchietti, L., Cierpicki, T., Xue, F., MacKerell, A. D., & Melnick, A. M.
Affiliations: University of Maryland, Baltimore (US)
University of California, San Francisco (US)
Weill Cornell Medicine (US)
University of Michigan (US)
ORCID: Yu, Wenbo
Geng, Huimin
Hatzi, Katerina
Shaknovich, Rita
Vanommeslaeghe, Kenno
Cheng, Huimin
Liang, Dongdong
Cho, Hyo Je
Abbott, Joshua
Tam, Wayne
Leonard, John P.
Elemento, Olivier
Cerchietti, Leandro
Cierpicki, Tomasz
Xue, Fengtian
MacKerell, Alexander D.
Melnick, Ari M.
Venue: Journal of Clinical Investigation
Publisher: American Society for Clinical Investigation
Published: 2016-08-02
Volume: 126
Issue: 9
Pages: 3351-3362
ISSN: 0021-9738 (ISSN-L)
1558-8238
DOI: 10.1172/jci85795
PMC: PMC5004937
OpenAlex: W2505733981
Cited by: 176
References: 40
Citations by year: 2026: 6 · 2025: 16 · 2024: 19 · 2023: 14 · 2022: 25 · 2021: 16 · 2020: 21 · 2019: 18 · 2018: 20 · 2017: 16 · 2016: 5
FWCI: 18.18
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Journal of Clinical Investigation (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
eScholarship (California Digital Library) (submittedVersion)
VUBIR (Vrije Universiteit Brussel) (submittedVersion)
Funders: Samuel Waxman Cancer Research Foundation
Leukemia and Lymphoma Society
Weill Cornell Medical College
National Cancer Institute (R01CA194547)
Topics: Health Sciences › Medicine › Pathology and Forensic Medicine › Lymphoma Diagnosis and Treatment
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
Health Sciences › Medicine › Hematology › Chronic Lymphocytic Leukemia Research
Keywords: BCL6, small molecule inhibitors, germinal center, chromosomal translocation, lymphoma treatment
MeSH terms: Animals, Antineoplastic Agents, Doxorubicin, Drug Screening Assays, Antitumor, Humans, Indoles, Ligands, Male, Neoplasm Transplantation, Magnetic Resonance Spectroscopy, Protein Binding, Translocation, Genetic, Drug Design, Gene Expression Regulation, Neoplastic, Lymphoma, Large B-Cell, Diffuse, Mice, SCID, Thiazolidinediones, Cell Line, Tumor, Mice, Proto-Oncogene Proteins c-bcl-6, HEK293 Cells

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Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma

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