PubRank

James E Bradner

Author PubWeight™ 175.71‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Selective inhibition of BET bromodomains. Nature 2010 18.79
2 BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell 2011 14.34
3 RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature 2011 11.44
4 Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies. Science 2007 10.60
5 Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell 2013 8.37
6 Transcriptional amplification in tumor cells with elevated c-Myc. Cell 2012 8.24
7 HDAC2 negatively regulates memory formation and synaptic plasticity. Nature 2009 6.96
8 PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res 2007 5.45
9 Direct inhibition of the NOTCH transcription factor complex. Nature 2009 4.82
10 The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science 2013 4.20
11 Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma. Proc Natl Acad Sci U S A 2005 3.86
12 Small-molecule inhibition of BRDT for male contraception. Cell 2012 3.50
13 Targeting MYCN in neuroblastoma by BET bromodomain inhibition. Cancer Discov 2013 3.11
14 BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. Blood 2012 2.91
15 Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia. Proc Natl Acad Sci U S A 2009 2.54
16 Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins. Proc Natl Acad Sci U S A 2012 2.52
17 The bromodomain protein Brd4 insulates chromatin from DNA damage signalling. Nature 2013 2.46
18 BET bromodomains mediate transcriptional pause release in heart failure. Cell 2013 2.17
19 Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition. Genes Dev 2013 2.12
20 Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors. Angew Chem Int Ed Engl 2007 2.11
21 Clinicopathologic features and long-term outcomes of NUT midline carcinoma. Clin Cancer Res 2012 2.06
22 HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans. J Clin Invest 2010 1.93
23 BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism. Cell Cycle 2012 1.88
24 Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol 2011 1.82
25 Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms. Blood 2014 1.68
26 Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun 2012 1.67
27 Differentiation of NUT midline carcinoma by epigenomic reprogramming. Cancer Res 2011 1.65
28 Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition. J Exp Med 2012 1.65
29 BET bromodomain inhibition of MYC-amplified medulloblastoma. Clin Cancer Res 2013 1.64
30 Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor. J Am Chem Soc 2008 1.64
31 Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells. Leuk Lymphoma 2011 1.59
32 Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer. Clin Cancer Res 2013 1.56
33 PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Res 2013 1.53
34 Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Oncotarget 2012 1.50
35 HDAC6 inhibition enhances 17-AAG--mediated abrogation of hsp90 chaperone function in human leukemia cells. Blood 2008 1.47
36 Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. J Med Chem 2009 1.42
37 Donor-recipient mismatch for common gene deletion polymorphisms in graft-versus-host disease. Nat Genet 2009 1.40
38 Structural origin of selectivity in class II-selective histone deacetylase inhibitors. J Med Chem 2008 1.34
39 Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole. J Am Chem Soc 2009 1.33
40 SD-1029 inhibits signal transducer and activator of transcription 3 nuclear translocation. Clin Cancer Res 2006 1.32
41 Lymphocyte chemotaxis is regulated by histone deacetylase 6, independently of its deacetylase activity. Mol Biol Cell 2006 1.29
42 Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL. Cell 2012 1.26
43 c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells. Blood 2014 1.23
44 Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold. Org Lett 2009 1.23
45 Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells. Mol Cancer Ther 2014 1.18
46 On the inhibition of histone deacetylase 8. Bioorg Med Chem 2010 1.18
47 Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia. J Clin Invest 2014 1.17
48 In vivo pharmacodynamic imaging of proteasome inhibition. Mol Imaging 2009 1.16
49 Targeting transcription factor SALL4 in acute myeloid leukemia by interrupting its interaction with an epigenetic complex. Blood 2013 1.15
50 Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2. Mol Cancer Ther 2014 1.09
51 Recruitment of Brd4 to the human papillomavirus type 16 DNA replication complex is essential for replication of viral DNA. J Virol 2013 1.07
52 Tubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis. J Biol Chem 2009 1.07
53 BET acetyl-lysine binding proteins control pathological cardiac hypertrophy. J Mol Cell Cardiol 2013 1.04
54 Discovery of histone deacetylase 8 selective inhibitors. Bioorg Med Chem Lett 2011 0.99
55 A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas. J Clin Invest 2013 0.99
56 Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma. Int J Cancer 2014 0.97
57 Protection from UV-induced skin carcinogenesis by genetic inhibition of the ataxia telangiectasia and Rad3-related (ATR) kinase. Proc Natl Acad Sci U S A 2011 0.95
58 RapidCaP, a novel GEM model for metastatic prostate cancer analysis and therapy, reveals myc as a driver of Pten-mutant metastasis. Cancer Discov 2014 0.93
59 Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation. Chem Biol 2013 0.92
60 Biased multicomponent reactions to develop novel bromodomain inhibitors. J Med Chem 2014 0.87
61 Bromodomain and extraterminal (BET) protein inhibition suppresses human T cell leukemia virus 1 (HTLV-1) Tax protein-mediated tumorigenesis by inhibiting nuclear factor κB (NF-κB) signaling. J Biol Chem 2013 0.87
62 Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. Bioorg Med Chem Lett 2013 0.85
63 Intracellular protein degradation and its therapeutic implications. Clin Cancer Res 2005 0.85
64 Effect of thrombocytopenia on outcomes following treatment with either enoxaparin or unfractionated heparin in patients presenting with acute coronary syndromes. Am J Cardiol 2007 0.81
65 Pre-clinical analysis of changes in intra-cellular biochemistry of glioblastoma multiforme (GBM) cells due to c-Myc silencing. Cell Mol Neurobiol 2014 0.79
66 Comparative pharmacokinetic properties and antitumor activity of the marine HDACi Largazole and Largazole peptide isostere. Cancer Chemother Pharmacol 2015 0.78
67 A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorg Med Chem Lett 2011 0.78
68 Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors. ACS Med Chem Lett 2011 0.77
69 A pulse at the heart of targeted therapy. Nat Chem Biol 2009 0.75
70 A chemical probe toolbox for dissecting the cancer epigenome. Nat Rev Cancer 2017 0.75
71 Correction: Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells. PLoS One 2015 0.75
72 Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. J Med Chem 2017 0.75
73 A cyclodextrin-capped histone deacetylase inhibitor. Bioorg Med Chem Lett 2013 0.75
74 Interview with James Bradner. Interviewed by Hannah Coaker. Future Med Chem 2013 0.75