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Items: 16


RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease.

Jahagirdar R, Attwell S, Marusic S, Bendele A, Shenoy N, McLure KG, Gilham D, Norek K, Hansen HC, Yu R, Tobin J, Wagner GS, Young PR, Wong NCW, Kulikowski E.

Mol Pharmacol. 2017 Dec;92(6):694-706. doi: 10.1124/mol.117.110379. Epub 2017 Sep 29.


Data on gene and protein expression changes induced by apabetalone (RVX-208) in ex vivo treated human whole blood and primary hepatocytes.

Wasiak S, Gilham D, Tsujikawa LM, Halliday C, Norek K, Patel RG, McLure KG, Young PR, Gordon A, Kulikowski E, Johansson J, Sweeney M, Wong NC.

Data Brief. 2016 Jul 29;8:1280-8. doi: 10.1016/j.dib.2016.07.047. eCollection 2016 Sep.


RVX-297- a novel BD2 selective inhibitor of BET bromodomains.

Kharenko OA, Gesner EM, Patel RG, Norek K, White A, Fontano E, Suto RK, Young PR, McLure KG, Hansen HC.

Biochem Biophys Res Commun. 2016 Aug 12;477(1):62-7. doi: 10.1016/j.bbrc.2016.06.021. Epub 2016 Jun 6.


Small molecule screen for inhibitors of expression from canonical CREB response element-containing promoters.

Mitton B, Hsu K, Dutta R, Tiu BC, Cox N, McLure KG, Chae HD, Smith M, Eklund EA, Solow-Cordero DE, Sakamoto KM.

Oncotarget. 2016 Feb 23;7(8):8653-62. doi: 10.18632/oncotarget.7085.


BET bromodomain inhibitors synergize with ATR inhibitors to induce DNA damage, apoptosis, senescence-associated secretory pathway and ER stress in Myc-induced lymphoma cells.

Muralidharan SV, Bhadury J, Nilsson LM, Green LC, McLure KG, Nilsson JA.

Oncogene. 2016 Sep 8;35(36):4689-97. doi: 10.1038/onc.2015.521. Epub 2016 Jan 25.


Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.

Duffy BC, Liu S, Martin GS, Wang R, Hsia MM, Zhao H, Guo C, Ellis M, Quinn JF, Kharenko OA, Norek K, Gesner EM, Young PR, McLure KG, Wagner GS, Lakshminarasimhan D, White A, Suto RK, Hansen HC, Kitchen DB.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2818-23. doi: 10.1016/j.bmcl.2015.04.107. Epub 2015 May 11.


A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.

Jahagirdar R, Zhang H, Azhar S, Tobin J, Attwell S, Yu R, Wu J, McLure KG, Hansen HC, Wagner GS, Young PR, Srivastava RA, Wong NC, Johansson J.

Atherosclerosis. 2014 Sep;236(1):91-100. doi: 10.1016/j.atherosclerosis.2014.06.008. Epub 2014 Jun 28.


BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma.

Bhadury J, Nilsson LM, Muralidharan SV, Green LC, Li Z, Gesner EM, Hansen HC, Keller UB, McLure KG, Nilsson JA.

Proc Natl Acad Sci U S A. 2014 Jul 1;111(26):E2721-30. doi: 10.1073/pnas.1406722111. Epub 2014 Jun 16.


RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.

McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E, Suto RK, Wong NC, Wagner GS, Hansen HC, Young PR.

PLoS One. 2013 Dec 31;8(12):e83190. doi: 10.1371/journal.pone.0083190. eCollection 2013.


Regulation of p53 translation and induction after DNA damage by ribosomal protein L26 and nucleolin.

Takagi M, Absalon MJ, McLure KG, Kastan MB.

Cell. 2005 Oct 7;123(1):49-63. Erratum in: Cell. 2005 Nov 4;123(3):536-7.


NAD+ modulates p53 DNA binding specificity and function.

McLure KG, Takagi M, Kastan MB.

Mol Cell Biol. 2004 Nov;24(22):9958-67.


DNA-dependent protein kinase acts upstream of p53 in response to DNA damage.

Woo RA, McLure KG, Lees-Miller SP, Rancourt DE, Lee PW.

Nature. 1998 Aug 13;394(6694):700-4.


How p53 binds DNA as a tetramer.

McLure KG, Lee PW.

EMBO J. 1998 Jun 15;17(12):3342-50.


A PAb240+ conformation of wild type p53 binds DNA.

McLure KG, Lee PW.

Oncogene. 1996 Sep 19;13(6):1297-303.


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