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James Bradner

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Chemicals & Drugs

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Acetylation

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Jahangir Amin; James E Bradner; James Clarke; John Milton; Ronald M Paranal; Antonino Puglisi; Minghua Wang; John Spencer
A cyclodextrin-capped histone deacetylase inhibitor.
Jakob Lovén; David A Orlando; Christopher R Vakoc; James E Bradner; Heather A Hoke; Ashley Lau; Tong Ihn Lee; Charles Y Lin; Richard A Young
Selective inhibition of tumor oncogenes by disruption of super-enhancers.
Alexandre Puissant; Jun Qi; William A Weiss; Rhamy Zeid; Gabriela Alexe; Christopher F Bassil; Cyril H Benes; James E Bradner; Yvan H Chanthery; Stacey M Frumm; Matthew J Garnett; Patricia Greninger; William Clay Gustafson; Andrew L Kung; Ultan McDermott; Erin A Nekritz; Kimberly Stegmaier
Targeting MYCN in neuroblastoma by BET bromodomain inhibition.

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All Publications

2013: Jahangir Amin; James E Bradner; James Clarke; John Milton; Ronald M Paranal; Antonino Puglisi; Minghua Wang; John Spencer
A cyclodextrin-capped histone deacetylase inhibitor.
Bioorganic & medicinal chemistry letters 2013;23(11):3346-8.
2013: Jakob Lovén; David A Orlando; Christopher R Vakoc; James E Bradner; Heather A Hoke; Ashley Lau; Tong Ihn Lee; Charles Y Lin; Richard A Young
Selective inhibition of tumor oncogenes by disruption of super-enhancers.
Cell 2013;153(2):320-34.
2013: Alexandre Puissant; Jun Qi; William A Weiss; Rhamy Zeid; Gabriela Alexe; Christopher F Bassil; Cyril H Benes; James E Bradner; Yvan H Chanthery; Stacey M Frumm; Matthew J Garnett; Patricia Greninger; William Clay Gustafson; Andrew L Kung; Ultan McDermott; Erin A Nekritz; Kimberly Stegmaier
Targeting MYCN in neuroblastoma by BET bromodomain inhibition.
Cancer discovery 2013;3(3):308-23.
2013: Daniela Boehm; James E Bradner; Vincenzo Calvanese; Roy D Dar; Pao-Chen Li; Laura Martins; Vicente Planelles; Sebastian Schroeder; Robert Siliciano; Eric Verdin; Leor Weinberger; Sifei Xing; Ming-Ming Zhou; Katherine Aull; Melanie Ott
BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism.
Cell cycle (Georgetown, Tex.) 2013;12(3):452-62.
2012: Harald Herrmann; Hans-Peter Horny; Leonhard Müllauer; Junwei Shi; Wolfgang R Sperr; Christopher R Vakoc; Katharina Blatt; James E Bradner; Sabine Cerny-Reiterer; Karoline V Gleixner; Johannes Zuber; Peter Valent
Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.
Oncotarget 2012;3(12):1588-99.
2012: William W Lockwood; James E Bradner; Kreshnik Zejnullahu; Harold Varmus
Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins.
Proceedings of the National Academy of Sciences of the United States of America 2012;109(47):19408-13.
2012: Christopher J Ott; Ronald M Paranal; Jun Qi; Scott Rodig; Liat Bird; Teresa Bowman; James E Bradner; Nadja Kopp; Andrew L Kung; David M Weinstock
BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.
Blood 2012;120(14):2843-52.
2012: Charles Y Lin; Jakob Lovén; Ronald M Paranal; Peter B Rahl; James E Bradner; Christopher B Burge; Tong Ihn Lee; Richard A Young
Transcriptional amplification in tumor cells with elevated c-Myc.
Cell 2012;151(1):56-67.
2012: Martin M Matzuk; Michael R McKeown; Sarah Picaud; Jun Qi; Richard N Yu; Panagis Filippakopoulos; Stefan Knapp; Madeleine E Lemieux; Qinglei Li; Lang Ma; Julio E Agno; James E Bradner
Small-molecule inhibition of BRDT for male contraception.
Cell 2012;150(4):673-84.
2012: Loredana Santo; Tyler Scullen; David Tamang; Jen-Chieh Tseng; John H van Duzer; Min Yang; Scott Rodig; Kenneth C Anderson; James E Bradner; Miriam Canavese; Diana Cirstea; Homare Eda; Teru Hideshima; Matthew Jarpe; Simon S Jones; Andrew L Kung; Ralph Mazitschek; Walter C Ogier; Noopur Raje
Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.
Blood 2012;119(11):2579-89.
2012: Wenyu Yu; Alex Scopton; Tatiana Shatseva; Wolfram Tempel; Masoud Vedadi; Amy K Wernimont; Erno Wienholds; Joanna Yi; Rima Al-Awar; Ahmed Aman; Cheryl H Arrowsmith; Dalia Barsyte-Lovejoy; James E Bradner; Peter J Brown; Emma J Chory; John E Dick; John R Engen; Guillermina Estiu; Alexander Federation; Carly Griffin; Taraneh Hajian; Roxana E Iacob; Fengling Li; Richard Marcellus; Jason J Marineau; Javier Pineda; Jun Qi; Matthieu Schapira
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Nature communications 2012;3():1288.
2011: Johannes Zuber; Peter Valent; Eric Wang; Mark Wunderlich; Katharina Blatt; James E Bradner; Patrick Brown; Agustin Chicas; Harald Herrmann; Christopher Johns; Scott C Kogan; Scott W Lowe; Daniel Magoon; James C Mulloy; Jun Qi; Amy R Rappaport; Junwei Shi; Edward Allan Racela Sison; Meredith J Taylor; Christopher R Vakoc
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
Nature 2011;478(7370):524-8.
2011: Jake E Delmore; Irene M Ghobrial; Timothy Gilpatrick; William C Hahn; Timothy P Heffernan; Ghayas C Issa; Hannah M Jacobs; Efstathios Kastritis; Andrew L Kung; Madeleine E Lemieux; Michael R McKeown; Ronald M Paranal; Jun Qi; Peter B Rahl; Paul G Richardson; Anna C Schinzel; Junwei Shi; Christopher R Vakoc; Richard A Young; Kenneth C Anderson; P Leif Bergsagel; James E Bradner; Marta Chesi; Constantine S Mitsiades
BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
Cell 2011;146(6):904-17.
2011: Masaoki Kawasumi; Yong-son Kim; Sang-wahn Koo; Bianca Lemos; Douglas Levine; Isabel Longo; Yao-Ping Lu; Anna Mandinova; Aimee Angle-Zahn; James E Bradner; Adam Chen; Allan H Conney; Timothy P Heffernan; Erin Higgins; Lynh Nguyen; Miranda Schmidt; Renee Thibodeau; Paul X Nghiem
Protection from UV-induced skin carcinogenesis by genetic inhibition of the ataxia telangiectasia and Rad3-related (ATR) kinase.
Proceedings of the National Academy of Sciences of the United States of America 2011;108(33):13716-21.
2011: Melissa M Kemp; James E Bradner; Jason H Fuller; Nicole M Martinez; Elizabeth M Morse; Stuart L Schreiber; Qiu Wang; Michel Weïwer; Nathan West; Angela N Koehler
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
Bioorganic & medicinal chemistry letters 2011;21(14):4164-9.
2010: Guillermina Estiu; Nathan West; Ralph Mazitschek; Edward Greenberg; James E Bradner; Olaf Wiest
On the inhibition of histone deacetylase 8.
Bioorganic & medicinal chemistry 2010;18(11):4103-10.
2010: Akinori Yoda; Yuka Yoda; Sabina Chiaretti; Michal Bar-Natan; Kartik Mani; Scott J Rodig; Nathan West; Yun Xiao; Jennifer R Brown; Constantine Mitsiades; Martin Sattler; Jeffery L Kutok; Daniel J DeAngelo; Martha Wadleigh; Alfonso Piciocchi; Paola Dal Cin; James E Bradner; James D Griffin; Kenneth C Anderson; Richard M Stone; Jerome Ritz; Robin Foà; Jon C Aster; David A Frank; David M Weinstock
Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia.
Proceedings of the National Academy of Sciences of the United States of America 2010;107(1):252-7.
2009: Steven A McCarroll; James E Bradner; Hannu Turpeinen; Liisa Volin; Paul J Martin; Shannon D Chilewski; Joseph H Antin; Stephanie J Lee; Tapani Ruutu; Barry Storer; Edus H Warren; Bo Zhang; Lue Ping Zhao; David Ginsburg; Robert J Soiffer; Jukka Partanen; John A Hansen; Jerome Ritz; Aarno Palotie; David Altshuler
Donor-recipient mismatch for common gene deletion polymorphisms in graft-versus-host disease.
Nature genetics 2009;41(12):1341-4.
2009: Albert A Bowers; Nathan West; Tenaya L Newkirk; Annie E Troutman-Youngman; Stuart L Schreiber; Olaf Wiest; James E Bradner; Robert M Williams
Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.
Organic letters 2009;11(6):1301-4.
2009: Albert A Bowers; Thomas J Greshock; Nathan West; Guillermina Estiu; Stuart L Schreiber; Olaf Wiest; Robert M Williams; James E Bradner
Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.
Journal of the American Chemical Society 2009;131(8):2900-5.
2008: Rekha Rao Manepalli; Warren C Fiskus; Yonghua Yang; Pearl Lee; Rajeshree Joshi; Pravina Fernandez; Aditya Mandawat; Peter Atadja; James E Bradner; Kapil N Bhalla
HDAC6 inhibition enhances 17-AAG--mediated abrogation of hsp90 chaperone function in human leukemia cells.
Blood 2008;112(5):1886-93.
2008: Albert Bowers; Nathan West; Jack Taunton; Stuart L Schreiber; James E Bradner; Robert M Williams
Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor.
Journal of the American Chemical Society 2008;130(33):11219-22.
2008: Guillermina Estiu; Edward Greenberg; Christopher B Harrison; Nicholas P Kwiatkowski; Ralph Mazitschek; James E Bradner; Olaf Wiest
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
Journal of medicinal chemistry 2008;51(10):2898-906.
2007: Jeffrey A Engelman; Kreshnik Zejnullahu; Christopher-Michael Gale; Eugene Lifshits; Andrea J Gonzales; Takeshi Shimamura; Feng Zhao; Patrick W Vincent; George N Naumov; James E Bradner; Irene W Althaus; Leena Gandhi; Geoffrey I Shapiro; James M Nelson; John V Heymach; Matthew Meyerson; Kwok-Kin Wong; Pasi A Janne
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Cancer research 2007;67(24):11924-32.
2007: Robert W Yeh; Stephen D Wiviott; Robert P Giugliano; David A Morrow; Amy Shui; Jie Qin; Benjamin M Scirica; James E Bradner; Ik-Kyung Jang; C Michael Gibson; Elliott M Antman
Effect of thrombocytopenia on outcomes following treatment with either enoxaparin or unfractionated heparin in patients presenting with acute coronary syndromes.
The American journal of cardiology 2007;100(12):1734-8.
2007: Zhenfeng Duan; James E Bradner; Edward Greenberg; Ralph Mazitschek; Rosemary Foster; Jennifer Mahoney; Michael Seiden
8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells.
Molecular pharmacology 2007;72(5):1137-45.
2007: Jayne M Stommel; Alec C Kimmelman; Haoqiang Ying; Roustem Nabioullin; Aditya H Ponugoti; Ruprecht Wiedemeyer; Alexander H Stegh; James E Bradner; Keith L Ligon; Cameron Brennan; Lynda Chin; Ronald A DePinho
Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies.
Science (New York, N.Y.) 2007;318(5848):287-90.
2007: Arturo J Vegas; James E Bradner; Weiping Tang; Olivia M McPherson; Edward F Greenberg; Angela N Koehler; Stuart L Schreiber
Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors.
Angewandte Chemie (International ed. in English) 2007;46(42):7960-4.
2006: Zhenfeng Duan; James E Bradner; Edward Greenberg; Ross Levine; Rosemary Foster; Jennifer Mahoney; Michael Seiden
SD-1029 inhibits signal transducer and activator of transcription 3 nuclear translocation.
Clinical cancer research : an official journal of the American Association for Cancer Research 2006;12(22):6844-52.
2006: J Román Cabrero; Juan M Serrador; Olga Barreiro; María Mittelbrunn; Salvador Naranjo-Suárez; Noa B Martín-Cófreces; Miguel Vicente-Manzanares; Ralph Mazitschek; James E Bradner; Jesús Avila; Agustín Valenzuela-Fernández; Francisco Sánchez-Madrid
Lymphocyte chemotaxis is regulated by histone deacetylase 6, independently of its deacetylase activity.
Molecular biology of the cell 2006;17(8):3435-45.
2006: James E Bradner; Olivia M McPherson; Ralph Mazitschek; David Barnes-Seeman; John P Shen; Jasmeet Dhaliwal; Kristen E Stevenson; Jay L Duffner; Seung Bum Park; Donna Neuberg; Paul X Nghiem; Stuart L Schreiber; Angela N Koehler
A robust small-molecule microarray platform for screening cell lysates.
Chemistry & biology 2006;13(5):493-504.
2006: James E Bradner; Olivia M McPherson; Angela N Koehler
A method for the covalent capture and screening of diverse small molecules in a microarray format.
Nature protocols 2006;1(5):2344-52.
2005: Teru Hideshima; James E Bradner; Dharminder Chauhan; Kenneth C Anderson
Intracellular protein degradation and its therapeutic implications.
Clinical cancer research : an official journal of the American Association for Cancer Research 2005;11(24 Pt 1):8530-3.
2005: Purva Bali; Michael Pranpat; James E Bradner; Maria Balasis; Warren C Fiskus; Fei Guo; Kathy Rocha; Sandhya Kumaraswamy; Sandhya Boyapalle; Peter Atadja; Edward Seto; Kapil N Bhalla
Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors.
The Journal of biological chemistry 2005;280(29):26729-34.
2005: Teru Hideshima; James E Bradner; Jason Wong; Dharminder Chauhan; Paul Richardson; Stuart L Schreiber; Kenneth C Anderson
Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma.
Proceedings of the National Academy of Sciences of the United States of America 2005;102(24):8567-72.
2001: Yanping Luo; S K Rockow-Magnone; Mary K Joseph; James E Bradner; C C Butler; Stephen K Tahir; Edward K Han; Shi-Chung Ng; Jean M Severin; Earl J Gubbins; R M Reilly; A Rueter; Robert L Simmer; Thomas F Holzman; Vincent L Giranda
Abrogation of G2 checkpoint specifically sensitize p53 defective cells to cancer chemotherapeutic agents.
Anticancer research 2001;21(1A):23-8.
1999: Patrick P Lin; R I Brody; AC Hamelin; James E Bradner; John Healey; Marc Ladanyi
Differential transactivation by alternative EWS-FLI1 fusion proteins correlates with clinical heterogeneity in Ewing's sarcoma.
Cancer research 1999;59(7):1428-32.