The DOI matches its Crossref record; 53 of the 53 references it cites were found in a registry or an index.
A Small-Molecule Inhibitor of BCL6 Kills DLBCL Cells In Vitro and In Vivo
Open accessAbstract
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.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
In the citing paper
“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]
In the citing paper
“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]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Berman, H. M. (2000) · Nucleic Acids Research · doi:10.1093/nar/28.1.235 · Cited by 40,196
Coot : model-building tools for molecular graphics
Emsley, P., & Cowtan, K. (2004) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444904019158 · Cited by 30,571
Phaser crystallographic software
McCoy, A. J., Grosse-Kunstleve, R. W., Adams, P. D., Winn, M. D., Storoni, L. C., & Read, R. J. (2007) · Journal of Applied Crystallography · doi:10.1107/s0021889807021206 · Cited by 20,612
The PyMOL Molecular Graphics System
DeLano, W. L. (2002) · Medical Entomology and Zoology · Cited by 18,147
Crystallography & NMR System: A New Software Suite for Macromolecular Structure Determination
Brünger, A. T., Adams, P. D., Clore, G. M., DeLano, W. L., Gros, P., Grosse‐Kunstleve, R. W., Jiang, J., Kuszewski, J. J., Nilges, M., Pannu, N., et al. (1998) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444998003254 · Cited by 15,723
Refinement of Macromolecular Structures by the Maximum-Likelihood Method
Murshudov, G. N., Vagin, A. A., & Dodson, E. J. (1997) · Acta Crystallographica Section D Biological Crystallography · doi:10.1107/s0907444996012255 · Cited by 14,796
All-Atom Empirical Potential for Molecular Modeling and Dynamics Studies of Proteins
MacKerell, A. D., Bashford, D., Bellott, M., Dunbrack, R. L., Evanseck, J. D., Field, M. J., Fischer, S., Gao, J., Guo, H., Ha, S., et al. (1998) · The Journal of Physical Chemistry B · doi:10.1021/jp973084f · Cited by 14,429
Self-citationCHARMM: A program for macromolecular energy, minimization, and dynamics calculations
Brooks, B., Bruccoleri, R., Olafson, B. D., States, D., Swaminathan, S., & Karplus, M. (1983) · Journal of Computational Chemistry · doi:10.1002/jcc.540040211 · Cited by 13,736
Drug-like properties and the causes of poor solubility and poor permeability
Lipinski, C. A. (2000) · Journal of Pharmacological and Toxicological Methods · doi:10.1016/s1056-8719(00)00107-6 · Cited by 3,776
A geometric approach to macromolecule-ligand interactions
Kuntz, I. D., Blaney, J. M., Oatley, S. J., Langridge, R., & Ferrin, T. E. (1982) · Journal of Molecular Biology · doi:10.1016/0022-2836(82)90153-x · Cited by 2,287
Cited by
Sorted by citations
Computational Methods in Drug Discovery
Sliwoski, G. R., Kothiwale, S., Meiler, J., & Lowe, E. W. (2013) · Pharmacological Reviews · doi:10.1124/pr.112.007336 · Cited by 2,306
Sehn, L. H., & Gascoyne, R. D. (2014) · Blood · doi:10.1182/blood-2014-05-577189 · Cited by 581
Rubenstein, J. L., Hsi, E. D., Johnson, J. L., Jung, S., Nakashima, M. O., Grant, B., Cheson, B. D., & Kaplan, L. D. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.46.9957 · Cited by 506
Relapsed/Refractory Diffuse Large B-Cell Lymphoma
Friedberg, J. W. (2011) · Hematology · doi:10.1182/asheducation-2011.1.498 · Cited by 499
Pathogenesis of Human B Cell Lymphomas
Shaffer, A. L., Young, R. M., & Staudt, L. M. (2012) · Annual Review of Immunology · doi:10.1146/annurev-immunol-020711-075027 · Cited by 457
Metadata
- 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
- 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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
