ArticleThe Journal of clinical investigation2016
Rationally designed BCL6 inhibitors target activated B cell diffuse large B cell lymphoma.
Article in The Journal of clinical investigation, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 97 papers.
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Who cites it
97 citing papers in PubMed, 172 citations in OpenAlex.
- Mouse models of B cell lymphomas on the basis of genetic features.Frontiers in immunology · 2026Review
- SOX11 modulates BCR signaling through the PAX5/CD19 axis for therapeutic targeting in BTK-resistant mantle cell lymphoma.Blood advances · 2025Article
- Design and synthesis of novelFuture medicinal chemistry · 2025Article
- Bcl6 controls the stability and suppressive function of regulatory T cells in head and neck squamous cell carcinoma.Genes & diseases · 2025Article
- Type 1 Diabetes Depends on CD4-Driven Expression of the Transcriptional Repressor Bcl6.Diabetes · 2025Article
- Resveratrol as a BCL6 natural inhibitor suppresses germinal center derived Non-Hodgkin lymphoma cells growth.Journal of natural medicines · 2025Article
- Advances in pyrazolo[1,5-RSC advances · 2025Review
- Targeting RAB7 in human B lymphoma by a small molecule inhibitor arrests tumor cell growth.Frontiers in oncology · 2025Article
- Inhibitior of Bcl6 by FX1 protects DSS induced colitis mice through anti-inflammatory effects.Frontiers in immunology · 2025Article
- BCL6 inhibition: a promising approach to prevent germinal center-driven allo-immune responses.Frontiers in immunology · 2025Review
- How CBX proteins regulate normal and leukemic blood cells.FEBS letters · 2024Review
- B Cell Lymphoma 6 (BCL6): A Conserved Regulator of Immunity and Beyond.International journal of molecular sciences · 2024Review
- Pharmaceutical inhibition of BCL6 ameliorates resistance to imatinib in chronic myeloid leukemia.Heliyon · 2024Article
- The F-box E3 ligase protein FBXO11 regulates EBNA3C-associated degradation of BCL6.Journal of virology · 2024Article
- SMARCA4 is a haploinsufficient B cell lymphoma tumor suppressor that fine-tunes centrocyte cell fate decisions.Cancer cell · 2024Article
- Anti-PD-1 therapy triggers Tfh cell-dependent IL-4 release to boost CD8 T cell responses in tumor-draining lymph nodes.The Journal of experimental medicine · 2024Article
- Selective deletion of E3 ubiquitin ligase FBW7 in VE-cadherin-positive cells instigates diffuse large B-cell lymphoma in mice in vivo.Cell death & disease · 2024Article
- Transcriptional programming of translation by BCL6 controls skeletal muscle proteostasis.Nature metabolism · 2024Article
- Selectively targeting BCL6 using a small molecule inhibitor is a potential therapeutic strategy for ovarian cancer.International journal of biological sciences · 2024Article
- Determination of Ligand-Binding Affinity (Journal of medicinal chemistry · 2023Article
37 more citing papers are in PubMed but not listed here.
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Authors and funding
25 authors at 2 institutions in 1 country.
Funding
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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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.