A Study to Investigate the Safety, Pharmacokinetics, Pharmacodynamics, and Clinical Activity of GSK525762 in Subjects With NUT Midline Carcinoma (NMC) and Other Cancers

Clinical Trial ID NCT01587703

PubWeight™ 49.02‹?›

🔗 Visit the ClinicalTrials.gov page for NCT01587703

Top papers

Rank Title Journal Year PubWeight™‹?›
1 The mechanisms behind the therapeutic activity of BET bromodomain inhibition. Mol Cell 2014 2.47
2 The oncogenic BRD4-NUT chromatin regulator drives aberrant transcription within large topological domains. Genes Dev 2015 2.28
3 Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes. Science 2014 1.70
4 Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem 2012 1.55
5 Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol 2015 1.46
6 Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells. Elife 2015 1.46
7 NSD3-NUT fusion oncoprotein in NUT midline carcinoma: implications for a novel oncogenic mechanism. Cancer Discov 2014 1.27
8 Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia. Leukemia 2013 1.22
9 Cancer epigenetics drug discovery and development: the challenge of hitting the mark. J Clin Invest 2014 1.20
10 MYC, a downstream target of BRD-NUT, is necessary and sufficient for the blockade of differentiation in NUT midline carcinoma. Oncogene 2013 1.16
11 Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching. Epigenetics Chromatin 2014 1.14
12 Hijacked in cancer: the KMT2 (MLL) family of methyltransferases. Nat Rev Cancer 2015 1.12
13 RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One 2013 1.11
14 The importance of diagnosing NUT midline carcinoma. Head Neck Pathol 2013 1.10
15 Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence. Ther Adv Hematol 2015 1.06
16 Molecular Pathways: Targeting MYC-induced metabolic reprogramming and oncogenic stress in cancer. Clin Cancer Res 2013 1.04
17 BET bromodomain proteins are required for glioblastoma cell proliferation. Epigenetics 2014 0.99
18 Exploiting the Epigenome to Control Cancer-Promoting Gene-Expression Programs. Cancer Cell 2016 0.98
19 Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628. Cancer Discov 2016 0.97
20 NUT midline carcinoma: an aggressive intrathoracic neoplasm. J Thorac Oncol 2013 0.97
21 Inhibition of osteoclastogenesis and inflammatory bone resorption by targeting BET proteins and epigenetic regulation. Nat Commun 2014 0.96
22 Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity. J Neurosci 2015 0.96
23 Novel drug targets for personalized precision medicine in relapsed/refractory diffuse large B-cell lymphoma: a comprehensive review. Mol Cancer 2015 0.94
24 Small cell lung cancer: will recent progress lead to improved outcomes? Clin Cancer Res 2015 0.94
25 Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11. Br J Pharmacol 2014 0.94
26 Small molecules, big targets: drug discovery faces the protein-protein interaction challenge. Nat Rev Drug Discov 2016 0.93
27 Bromodomain inhibitors regulate the C9ORF72 locus in ALS. Exp Neurol 2015 0.91
28 Open access target validation is a more efficient way to accelerate drug discovery. PLoS Biol 2015 0.90
29 Targeting the histone orthography of cancer: drugs for writers, erasers and readers. Br J Pharmacol 2014 0.90
30 Genomic and Epigenomic Alterations in Cancer. Am J Pathol 2016 0.86
31 Clinical trials for BET inhibitors run ahead of the science. Drug Discov Today Technol 2016 0.86
32 Molecular profiling of childhood cancer: Biomarkers and novel therapies. BBA Clin 2014 0.86
33 Androgen receptor variant-driven prostate cancer: clinical implications and therapeutic targeting. Prostate Cancer Prostatic Dis 2016 0.83
34 Digging deep into "dirty" drugs - modulation of the methylation machinery. Drug Metab Rev 2015 0.83
35 Targeting MYCN: a good BET for improving neuroblastoma therapy? Cancer Discov 2013 0.83
36 Disruption of BRD4 at H3K27Ac-enriched enhancer region correlates with decreased c-Myc expression in Merkel cell carcinoma. Epigenetics 2015 0.83
37 Drugging Chromatin in Cancer: Recent Advances and Novel Approaches. Mol Cell 2015 0.81
38 BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma. Cancer Med 2016 0.80
39 Sarcoma Cell Line Screen of Oncology Drugs and Investigational Agents Identifies Patterns Associated with Gene and microRNA Expression. Mol Cancer Ther 2015 0.79
40 Gain-of-function mutation of chromatin regulators as a tumorigenic mechanism and an opportunity for therapeutic intervention. Curr Opin Oncol 2015 0.79
41 New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition. J Med Chem 2015 0.79
42 BET bromodomain-mediated interaction between ERG and BRD4 promotes prostate cancer cell invasion. Oncotarget 2016 0.77
43 Chemical synthesis of the ATAD2 bromodomain. Proc Natl Acad Sci U S A 2014 0.77
44 NUT Carcinoma of the Sublingual Gland. Head Neck Pathol 2015 0.77
45 Epigenetic Medicinal Chemistry. ACS Med Chem Lett 2015 0.77
46 Epigenetic modulators as therapeutic targets in prostate cancer. Clin Epigenetics 2016 0.76
47 Epigenetic Mechanisms Governing Innate Inflammatory Responses. J Interferon Cytokine Res 2016 0.76
48 Novel mechanism-based therapeutics for androgen axis blockade in castration-resistant prostate cancer. Curr Opin Endocrinol Diabetes Obes 2016 0.76
49 The molecular mechanics of mixed lineage leukemia. Oncogene 2016 0.76
50 Safety, pharmacokinetic, pharmacodynamic and clinical activity of molibresib for the treatment of nuclear protein in testis carcinoma and other cancers: Results of a Phase I/II open-label, dose escalation study. Int J Cancer 2021 0.75
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