James E Bradner

James E Bradner

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James E Bradner

James E Bradner

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Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.

ACS Med Chem Lett 2019 Oct 13;10(10):1443-1449. Epub 2019 Sep 13.

Department of Cancer Biology, Dana Farber Cancer Institute, Boston Massachusetts 02115, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.9b00243DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6792166PMC
October 2019

The BET inhibitor JQ1 attenuates double-strand break repair and sensitizes models of pancreatic ductal adenocarcinoma to PARP inhibitors.

EBioMedicine 2019 Jun 22;44:419-430. Epub 2019 May 22.

Department of Pharmacology and Toxicology, University of Alabama at Birmingham, 1670 University Blvd, Birmingham, AL, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ebiom.2019.05.035DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6604668PMC
June 2019

Enhancer Architecture and Essential Core Regulatory Circuitry of Chronic Lymphocytic Leukemia.

Cancer Cell 2018 12 29;34(6):982-995.e7. Epub 2018 Nov 29.

Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, 450 Brookline Avenue, Boston, MA 02115, USA; Department of Medicine, Harvard Medical School, Boston, MA 02115, USA; Broad Institute of MIT & Harvard, Cambridge, MA 02142, USA; Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S15356108183048
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http://dx.doi.org/10.1016/j.ccell.2018.11.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6298230PMC
December 2018

Non-overlapping Control of Transcriptome by Promoter- and Super-Enhancer-Associated Dependencies in Multiple Myeloma.

Cell Rep 2018 12;25(13):3693-3705.e6

Jerome Lipper Multiple Myeloma Center, Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02215, USA; VA Boston Healthcare System, Boston, MA, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2018.12.016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6407615PMC
December 2018

Combined BET bromodomain and CDK2 inhibition in MYC-driven medulloblastoma.

Oncogene 2018 05 7;37(21):2850-2862. Epub 2018 Mar 7.

Department of Immunology, Genetics and Pathology, Science for Life Laboratory, Rudbeck Laboratory, Uppsala University, Uppsala, Sweden.

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http://dx.doi.org/10.1038/s41388-018-0135-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5966365PMC
May 2018

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders.

ACS Chem Biol 2018 03 29;13(3):553-560. Epub 2018 Jan 29.

CeMM Research Center for Molecular Medicine of the Austrian Academy of Science , Lazarettgasse 14, AKH Bt. 25.3 , 1090 Vienna , Austria.

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http://pubs.acs.org/doi/10.1021/acschembio.7b00969
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http://dx.doi.org/10.1021/acschembio.7b00969DOI Listing
March 2018

BET bromodomain proteins regulate enhancer function during adipogenesis.

Proc Natl Acad Sci U S A 2018 02 14;115(9):2144-2149. Epub 2018 Feb 14.

Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115;

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http://dx.doi.org/10.1073/pnas.1711155115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5834672PMC
February 2018

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

Cell Chem Biol 2018 01 9;25(1):88-99.e6. Epub 2017 Nov 9.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S24519456173038
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http://dx.doi.org/10.1016/j.chembiol.2017.10.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427047PMC
January 2018

R-2HG Exhibits Anti-tumor Activity by Targeting FTO/mA/MYC/CEBPA Signaling.

Cell 2018 01 14;172(1-2):90-105.e23. Epub 2017 Dec 14.

Department of Cancer Biology, University of Cincinnati, Cincinnati, OH 45219, USA; Gehr Family Center for Leukemia Research, City of Hope, 1500 E. Duarte Rd., Duarte, CA 91010, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2017.11.031DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5766423PMC
January 2018

Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms.

Cancer Cell 2018 01 14;33(1):29-43.e7. Epub 2017 Dec 14.

Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, Box 20, New York, NY 10065, USA; Center for Epigenetics Research, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA; Center for Hematologic Malignancies, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA; Leukemia Service, Department of Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2017.11.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5760343PMC
January 2018

Therapeutic targeting of ependymoma as informed by oncogenic enhancer profiling.

Nature 2018 01 20;553(7686):101-105. Epub 2017 Dec 20.

Department of Stem Cell Biology and Regenerative Medicine, Lerner Research Institute, Cleveland Clinic, Cleveland, Ohio 44195, USA.

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http://dx.doi.org/10.1038/nature25169DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5993422PMC
January 2018

YY1 Is a Structural Regulator of Enhancer-Promoter Loops.

Cell 2017 Dec 7;171(7):1573-1588.e28. Epub 2017 Dec 7.

Whitehead Institute for Biomedical Research, Cambridge, MA 02142, USA; Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02142, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2017.11.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5785279PMC
December 2017

HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer.

Oncotarget 2017 Oct 5;8(46):80109-80123. Epub 2017 Jul 5.

Department of Medical Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA, USA.

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http://dx.doi.org/10.18632/oncotarget.19019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5655183PMC
October 2017

Bromodomain inhibition shows antitumoral activity in mice and human luminal breast cancer.

Oncotarget 2017 Aug 29;8(31):51621-51629. Epub 2017 May 29.

Cancer Epigenetics and Biology Program (PEBC), Bellvitge Biomedical Research Institute (IDIBELL), Barcelona, Catalonia, Spain.

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http://dx.doi.org/10.18632/oncotarget.18255DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5584274PMC
August 2017

ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia.

Nature 2017 03 1;543(7644):265-269. Epub 2017 Mar 1.

Department of Epigenetics and Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA.

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http://dx.doi.org/10.1038/nature21687DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5372383PMC
March 2017

Transcriptional Addiction in Cancer.

Cell 2017 02;168(4):629-643

Whitehead Institute for Biomedical Research, 9 Cambridge Center, Cambridge, MA 02142, USA; Department of Biology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2016.12.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5308559PMC
February 2017

A chemical probe toolbox for dissecting the cancer epigenome.

Nat Rev Cancer 2017 02;17(3):160-183

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts 02215, USA.

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http://dx.doi.org/10.1038/nrc.2016.148DOI Listing
February 2017

Inhibition of BET proteins and epigenetic signaling as a potential treatment for osteoporosis.

Bone 2017 01 23;94:10-21. Epub 2016 Sep 23.

INSERM, UMR 957, équipe labellisée ligue 2012, 1 Rue Gaston Veil, 44035 Nantes, France; Physiopathologie de la Résorption Osseuse et Thérapie des Tumeurs Osseuses Primitives, Université de Nantes, Nantes Atlantique Universités, EA3822, 1 Rue Gaston Veil, 44035 Nantes, France. Electronic address:

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http://dx.doi.org/10.1016/j.bone.2016.09.020DOI Listing
January 2017

Design and characterization of bivalent BET inhibitors.

Nat Chem Biol 2016 Dec 24;12(12):1089-1096. Epub 2016 Oct 24.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts, USA.

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http://dx.doi.org/10.1038/nchembio.2209DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5117811PMC
December 2016

Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET.

ChemMedChem 2016 Dec 15;11(23):2575-2581. Epub 2016 Nov 15.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, 02215, USA.

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http://dx.doi.org/10.1002/cmdc.201600502DOI Listing
December 2016

Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2.

Cancer Discov 2016 11 14;6(11):1237-1247. Epub 2016 Sep 14.

Division of Hematology/Oncology, Boston Children's Hospital and Department of Pediatric Oncology, Dana-Farber Cancer Institute, Harvard Stem Cell Institute, Harvard Medical School, Boston, Massachusetts.

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http://dx.doi.org/10.1158/2159-8290.CD-15-1439DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5096974PMC
November 2016

Targeting Chromatin Regulators Inhibits Leukemogenic Gene Expression in NPM1 Mutant Leukemia.

Cancer Discov 2016 10 17;6(10):1166-1181. Epub 2016 Aug 17.

Cancer Biology and Genetics Program, Memorial Sloan Kettering Cancer Center, New York, New York. Department of Pediatric Oncology, Dana-Farber Cancer Institute, and Division of Hematology/Oncology, Boston Children's Hospital, Harvard Medical School, Boston, Massachusetts.

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http://dx.doi.org/10.1158/2159-8290.CD-16-0237DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5584808PMC
October 2016

Development of a Potent and Selective HDAC8 Inhibitor.

ACS Med Chem Lett 2016 Oct 1;7(10):929-932. Epub 2016 Sep 1.

Department of Chemistry and Center for Molecular Discovery (BU-CMD), Boston University , 590 Commonwealth Avenue, Boston, Massachusetts 02215, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.6b00239DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5066159PMC
October 2016

Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer.

Cancer Discov 2016 09 16;6(9):1006-21. Epub 2016 Jun 16.

Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts. Department of Medicine, Harvard Medical School, Boston, Massachusetts. Belfer Institute for Applied Cancer Science, Dana-Farber Cancer Institute, Boston, Massachusetts.

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http://dx.doi.org/10.1158/2159-8290.CD-16-0164DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5010480PMC
September 2016

BET Inhibition Induces Apoptosis in Aggressive B-Cell Lymphoma via Epigenetic Regulation of BCL-2 Family Members.

Mol Cancer Ther 2016 09 12;15(9):2030-41. Epub 2016 Jul 12.

Gene Regulation Laboratory, Research Division, Peter MacCallum Cancer Centre, Melbourne, Victoria, Australia. Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, Victoria, Australia.

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http://dx.doi.org/10.1158/1535-7163.MCT-15-0924DOI Listing
September 2016

Mechanism, Consequences, and Therapeutic Targeting of Abnormal IL15 Signaling in Cutaneous T-cell Lymphoma.

Cancer Discov 2016 09 15;6(9):986-1005. Epub 2016 Jul 15.

Comprehensive Cancer Center, James Cancer Hospital and Solove Research Institute, The Ohio State University, Columbus, Ohio. Division of Hematology, Department of Internal Medicine, The Ohio State University, Columbus, Ohio.

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http://dx.doi.org/10.1158/2159-8290.CD-15-1297DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5388135PMC
September 2016

Signal-Dependent Recruitment of BRD4 to Cardiomyocyte Super-Enhancers Is Suppressed by a MicroRNA.

Cell Rep 2016 08 14;16(5):1366-1378. Epub 2016 Jul 14.

Division of Cardiology, Department of Medicine, University of Colorado Denver, Aurora, CO 80045, USA; Medical Scientist Training Program, University of Colorado Denver, Aurora, CO 80045, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2016.06.074DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4972677PMC
August 2016

High-Resolution Mapping of RNA Polymerases Identifies Mechanisms of Sensitivity and Resistance to BET Inhibitors in t(8;21) AML.

Cell Rep 2016 08 4;16(7):2003-16. Epub 2016 Aug 4.

Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA; Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2016.07.032DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4996374PMC
August 2016

Ligand-Promoted Meta-C-H Arylation of Anilines, Phenols, and Heterocycles.

J Am Chem Soc 2016 07 19;138(29):9269-76. Epub 2016 Jul 19.

Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.

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http://dx.doi.org/10.1021/jacs.6b04966DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5512281PMC
July 2016

BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma.

Cancer Med 2016 06 11;5(6):1183-93. Epub 2016 May 11.

Department of Pathology, New York University School of Medicine, New York, New York.

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http://dx.doi.org/10.1002/cam4.667DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4867668PMC
June 2016

The Bromodomain Inhibitor JQ1 and the Histone Deacetylase Inhibitor Panobinostat Synergistically Reduce N-Myc Expression and Induce Anticancer Effects.

Clin Cancer Res 2016 05 5;22(10):2534-44. Epub 2016 Jan 5.

Children's Cancer Institute Australia, Lowy Cancer Research Centre, University of New South Wales Australia, Randwick, New South Wales, Australia. School of Women's & Children's Health, University of New South Wales Australia, Randwick, New South Wales, Australia.

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http://dx.doi.org/10.1158/1078-0432.CCR-15-1666DOI Listing
May 2016

Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014).

Pharm Pat Anal 2015 ;4(4):261-84

Department of Medical Oncology, Dana-Farber Cancer Institute, 360 Longwood Avenue, Boston, MA 02215, USA.

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http://dx.doi.org/10.4155/ppa.15.16DOI Listing
April 2016

Models of human core transcriptional regulatory circuitries.

Genome Res 2016 Mar 3;26(3):385-96. Epub 2016 Feb 3.

Whitehead Institute for Biomedical Research, Cambridge, Massachusetts 02142, USA; Department of Biology, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA;

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http://dx.doi.org/10.1101/gr.197590.115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4772020PMC
March 2016

Functional Genomic Landscape of Human Breast Cancer Drivers, Vulnerabilities, and Resistance.

Cell 2016 Jan;164(1-2):293-309

Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 1L7, Canada; Laura and Isaac Perlmutter Cancer Centre, NYU-Langone Medical Center, NY 10016, USA. Electronic address:

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http://dx.doi.org/10.1016/j.cell.2015.11.062DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4724865PMC
January 2016

A Bead-Based Proximity Assay for BRD4 Ligand Discovery.

Curr Protoc Chem Biol 2015 Dec 2;7(4):263-278. Epub 2015 Dec 2.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.

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http://dx.doi.org/10.1002/9780470559277.ch150024DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4725578PMC
December 2015

Dose-dependent role of the cohesin complex in normal and malignant hematopoiesis.

J Exp Med 2015 Oct 5;212(11):1819-32. Epub 2015 Oct 5.

Human Oncology and Pathogenesis Program, Leukemia Service, Department of Medicine, Department of Pathology, Molecular Cytology Core Facility, and Center for Epigenetics Research, Memorial Sloan Kettering Cancer Center, New York, NY 10065 Human Oncology and Pathogenesis Program, Leukemia Service, Department of Medicine, Department of Pathology, Molecular Cytology Core Facility, and Center for Epigenetics Research, Memorial Sloan Kettering Cancer Center, New York, NY 10065 Human Oncology and Pathogenesis Program, Leukemia Service, Department of Medicine, Department of Pathology, Molecular Cytology Core Facility, and Center for Epigenetics Research, Memorial Sloan Kettering Cancer Center, New York, NY 10065

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http://dx.doi.org/10.1084/jem.20151317DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4612085PMC
October 2015

Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6.

Nucleic Acids Res 2015 Sep 27;43(16):7790-804. Epub 2015 Jun 27.

Department of Cell and Developmental Biology, University of Massachusetts Medical School, Worcester, MA 01655, USA

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http://dx.doi.org/10.1093/nar/gkv645DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4652747PMC
September 2015