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34233282
Synthesis of precursors of the agalacto (exo) fragment of the quartromicins via an auxiliary-controlled exo-selective Diels-Alder reaction.
Org Lett.
2006 Jun 22;8(13):2795-8. doi: 10.1021/ol0609208. PubMed PMID:
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Studies on the synthesis of quartromicins a(3) and d(3): synthesis of the vertical and horizontal bis-spirotetronate fragments.
J Org Chem.
2006 Sep 1;71(18):6915-22. doi: 10.1021/jo061059c. PubMed PMID:
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Total synthesis of (-)-himandrine.
J Am Chem Soc.
2009 Jul 22;131(28):9648-50. doi: 10.1021/ja903790y. PubMed PMID:
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Selective inhibition of BET bromodomains.
Nature.
2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. PubMed PMID:
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RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
Nature.
2011 Aug 3;478(7370):524-8. doi: 10.1038/nature10334. PubMed PMID:
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BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
Cell.
2011 Sep 16;146(6):904-17. doi: 10.1016/j.cell.2011.08.017. Epub 2011 Sep 1. PubMed PMID:
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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Nat Commun.
2012;3:1288. doi: 10.1038/ncomms2304. PubMed PMID:
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Small-molecule inhibition of BRDT for male contraception.
Cell.
2012 Aug 17;150(4):673-84. doi: 10.1016/j.cell.2012.06.045. PubMed PMID:
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BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.
Blood.
2012 Oct 4;120(14):2843-52. doi: 10.1182/blood-2012-02-413021. Epub 2012 Aug 17. PubMed PMID:
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Targeting MYCN in neuroblastoma by BET bromodomain inhibition.
Cancer Discov.
2013 Mar;3(3):308-23. doi: 10.1158/2159-8290.CD-12-0418. Epub 2013 Feb 21. PubMed PMID:
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Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.
Chem Biol.
2013 May 23;20(5):713-25. doi: 10.1016/j.chembiol.2013.03.020. PubMed PMID:
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BET bromodomains mediate transcriptional pause release in heart failure.
Cell.
2013 Aug 1;154(3):569-82. doi: 10.1016/j.cell.2013.07.013. PubMed PMID:
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BET acetyl-lysine binding proteins control pathological cardiac hypertrophy.
J Mol Cell Cardiol.
2013 Oct;63:175-9. doi: 10.1016/j.yjmcc.2013.07.017. Epub 2013 Aug 9. PubMed PMID:
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Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer.
Clin Cancer Res.
2013 Nov 15;19(22):6183-92. doi: 10.1158/1078-0432.CCR-12-3904. Epub 2013 Sep 17. PubMed PMID:
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Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma.
Cancer Cell.
2013 Dec 9;24(6):777-90. doi: 10.1016/j.ccr.2013.11.003. PubMed PMID:
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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 Dec 13;288(50):36094-105. doi: 10.1074/jbc.M113.485029. Epub 2013 Nov 4. PubMed PMID:
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Genome-wide localization of small molecules.
Nat Biotechnol.
2014 Jan;32(1):92-6. doi: 10.1038/nbt.2776. Epub 2013 Dec 15. PubMed PMID:
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c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells.
Blood.
2014 Feb 13;123(7):1040-50. doi: 10.1182/blood-2013-08-522698. Epub 2014 Jan 6. PubMed PMID:
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BET bromodomain inhibition of MYC-amplified medulloblastoma.
Clin Cancer Res.
2014 Feb 15;20(4):912-25. doi: 10.1158/1078-0432.CCR-13-2281. Epub 2013 Dec 2. PubMed PMID:
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RapidCaP, a novel GEM model for metastatic prostate cancer analysis and therapy, reveals myc as a driver of Pten-mutant metastasis.
Cancer Discov.
2014 Mar;4(3):318-33. doi: 10.1158/2159-8290.CD-13-0346. Epub 2014 Jan 20. PubMed PMID:
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Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms.
Blood.
2014 Mar 27;123(13):2075-83. doi: 10.1182/blood-2014-01-547760. Epub 2014 Jan 27. PubMed PMID:
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Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells.
Mol Cancer Ther.
2014 May;13(5):1142-54. doi: 10.1158/1535-7163.MCT-13-0770. Epub 2014 Jan 16. PubMed PMID:
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Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA.
Oncogene.
2014 May 1;33(18):2395-404. doi: 10.1038/onc.2013.179. Epub 2013 May 20. PubMed PMID:
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Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2.
Mol Cancer Ther.
2014 May;13(5):1194-205. doi: 10.1158/1535-7163.MCT-13-0341. Epub 2014 Jan 16. PubMed PMID:
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Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition.
Nat Med.
2014 Jul;20(7):732-40. doi: 10.1038/nm.3613. Epub 2014 Jun 29. PubMed PMID:
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Repression of BIM mediates survival signaling by MYC and AKT in high-risk T-cell acute lymphoblastic leukemia.
Leukemia.
2014 Sep;28(9):1819-27. doi: 10.1038/leu.2014.78. Epub 2014 Feb 20. PubMed PMID:
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BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD.
Mol Cancer Ther.
2014 Oct;13(10):2315-27. doi: 10.1158/1535-7163.MCT-14-0258. Epub 2014 Jul 22. PubMed PMID:
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Biased multicomponent reactions to develop novel bromodomain inhibitors.
J Med Chem.
2014 Nov 13;57(21):9019-27. doi: 10.1021/jm501120z. Epub 2014 Oct 31. PubMed PMID:
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Bromodomain and extraterminal domain inhibitors (BETi) for cancer therapy: chemical modulation of chromatin structure.
Cold Spring Harb Perspect Biol.
2014 Dec 1;6(12):a018663. doi: 10.1101/cshperspect.a018663. Review. PubMed PMID:
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Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects.
Cancer Res.
2014 Dec 15;74(24):7475-86. doi: 10.1158/0008-5472.CAN-14-0197. Epub 2014 Oct 15. PubMed PMID:
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Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014).
Pharm Pat Anal.
2015;4(4):261-84. doi: 10.4155/ppa.15.16. Review. PubMed PMID:
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Cytogenetic and clinical marks for defining high-risk myeloma in the context of bortezomib treatment.
Exp Hematol.
2015 Mar;43(3):168-176.e2. doi: 10.1016/j.exphem.2014.11.004. Epub 2014 Nov 20. PubMed PMID:
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Structure-guided DOT1L probe optimization by label-free ligand displacement.
ACS Chem Biol.
2015 Mar 20;10(3):667-74. doi: 10.1021/cb500796d. Epub 2015 Jan 15. PubMed PMID:
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DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia.
Nat Med.
2015 Apr;21(4):335-43. doi: 10.1038/nm.3832. Epub 2015 Mar 30. PubMed PMID:
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Acetylation site specificities of lysine deacetylase inhibitors in human cells.
Nat Biotechnol.
2015 Apr;33(4):415-23. doi: 10.1038/nbt.3130. Epub 2015 Mar 9. PubMed PMID:
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The impact of clone size on the prognostic value of chromosome aberrations by fluorescence in situ hybridization in multiple myeloma.
Clin Cancer Res.
2015 May 1;21(9):2148-56. doi: 10.1158/1078-0432.CCR-14-2576. Epub 2015 Feb 4. PubMed PMID:
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Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma.
Int J Cancer.
2015 May 1;136(9):2055-64. doi: 10.1002/ijc.29269. Epub 2014 Oct 30. PubMed PMID:
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Selective Inhibition of HDAC1 and HDAC2 as a Potential Therapeutic Option for B-ALL.
Clin Cancer Res.
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Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6.
Nucleic Acids Res.
2015 Sep 18;43(16):7790-804. doi: 10.1093/nar/gkv645. Epub 2015 Jun 27. PubMed PMID:
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Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib.
Blood.
2015 Sep 24;126(13):1565-74. doi: 10.1182/blood-2015-04-639542. Epub 2015 Aug 7. PubMed PMID:
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Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer.
Nature.
2016 Jan 21;529(7586):413-417. doi: 10.1038/nature16508. Epub 2016 Jan 6. PubMed PMID:
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HEXIM1 induction is mechanistically involved in mediating anti-AML activity of BET protein bromodomain antagonist.
Leukemia.
2016 Feb;30(2):504-8. doi: 10.1038/leu.2015.142. Epub 2015 Jun 15. PubMed PMID:
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The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models.
Oncogene.
2016 Feb 18;35(7):833-45. doi: 10.1038/onc.2015.126. Epub 2015 May 11. PubMed PMID:
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An oncogenic MYB feedback loop drives alternate cell fates in adenoid cystic carcinoma.
Nat Genet.
2016 Mar;48(3):265-72. doi: 10.1038/ng.3502. Epub 2016 Feb 1. PubMed PMID:
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Super enhancers at the miR-146a and miR-155 genes contribute to self-regulation of inflammation.
Biochim Biophys Acta.
2016 Apr;1859(4):564-71. doi: 10.1016/j.bbagrm.2016.02.004. Epub 2016 Feb 5. PubMed PMID:
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An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation.
Nat Med.
2016 Jun;22(6):632-40. doi: 10.1038/nm.4092. Epub 2016 May 2. PubMed PMID:
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Eradication of Acute Myeloid Leukemia with FLT3 Ligand-Targeted miR-150 Nanoparticles.
Cancer Res.
2016 Aug 1;76(15):4470-80. doi: 10.1158/0008-5472.CAN-15-2949. Epub 2016 Jun 8. PubMed PMID:
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Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer.
Cancer Discov.
2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PubMed PMID:
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Mechanism, Consequences, and Therapeutic Targeting of Abnormal IL15 Signaling in Cutaneous T-cell Lymphoma.
Cancer Discov.
2016 Sep;6(9):986-1005. doi: 10.1158/2159-8290.CD-15-1297. Epub 2016 Jul 15. PubMed PMID:
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