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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.

Bamborough P, Barnett HA, Becher I, Bird MJ, Chung CW, Craggs PD, Demont EH, Diallo H, Fallon DJ, Gordon LJ, Grandi P, Hobbs CI, Hooper-Greenhill E, Jones EJ, Law RP, Le Gall A, Lugo D, Michon AM, Mitchell DJ, Prinjha RK, Sheppard RJ, Watson AJ, Watson RJ.

ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092. eCollection 2016 Jun 9.


Molecular Pathways: Targeting the PI3K Pathway in Cancer-BET Inhibitors to the Rescue.

Stratikopoulos EE, Parsons RE.

Clin Cancer Res. 2016 Jun 1;22(11):2605-10. doi: 10.1158/1078-0432.CCR-15-2389.


A Novel Phenanthridionone Based Scaffold As a Potential Inhibitor of the BRD2 Bromodomain: Crystal Structure of the Complex.

Tripathi S, Mathur S, Deshmukh P, Manjula R, Padmanabhan B.

PLoS One. 2016 May 31;11(5):e0156344. doi: 10.1371/journal.pone.0156344. eCollection 2016.


BRD4 is a histone acetyltransferase that evicts nucleosomes from chromatin.

Devaiah BN, Case-Borden C, Gegonne A, Hsu CH, Chen Q, Meerzaman D, Dey A, Ozato K, Singer DS.

Nat Struct Mol Biol. 2016 Jun;23(6):540-8. doi: 10.1038/nsmb.3228. Epub 2016 May 9.


Segmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase A.

Williams FP, Milbradt AG, Embrey KJ, Bobby R.

PLoS One. 2016 Apr 29;11(4):e0154607. doi: 10.1371/journal.pone.0154607. eCollection 2016.


Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.

Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV.

J Med Chem. 2016 May 26;59(10):5095-101. doi: 10.1021/acs.jmedchem.5b01997. Epub 2016 May 11.


BRD4 Connects Enhancer Remodeling to Senescence Immune Surveillance.

Tasdemir N, Banito A, Roe JS, Alonso-Curbelo D, Camiolo M, Tschaharganeh DF, Huang CH, Aksoy O, Bolden JE, Chen CC, Fennell M, Thapar V, Chicas A, Vakoc CR, Lowe SW.

Cancer Discov. 2016 Jun;6(6):612-29. doi: 10.1158/2159-8290.CD-16-0217. Epub 2016 Apr 20.


BET Inhibition Attenuates Helicobacter pylori-Induced Inflammatory Response by Suppressing Inflammatory Gene Transcription and Enhancer Activation.

Chen J, Wang Z, Hu X, Chen R, Romero-Gallo J, Peek RM Jr, Chen LF.

J Immunol. 2016 May 15;196(10):4132-42. doi: 10.4049/jimmunol.1502261. Epub 2016 Apr 15.


Strategically targeting MYC in cancer.

Posternak V, Cole MD.

F1000Res. 2016 Mar 29;5. pii: F1000 Faculty Rev-408. doi: 10.12688/f1000research.7879.1. eCollection 2016. Review.


BET Bromodomain Inhibition Releases the Mediator Complex from Select cis-Regulatory Elements.

Bhagwat AS, Roe JS, Mok BY, Hohmann AF, Shi J, Vakoc CR.

Cell Rep. 2016 Apr 19;15(3):519-30. doi: 10.1016/j.celrep.2016.03.054. Epub 2016 Apr 7.


BET Bromodomain Suppression Inhibits VEGF-induced Angiogenesis and Vascular Permeability by Blocking VEGFR2-mediated Activation of PAK1 and eNOS.

Huang M, Qiu Q, Xiao Y, Zeng S, Zhan M, Shi M, Zou Y, Ye Y, Liang L, Yang X, Xu H.

Sci Rep. 2016 Apr 5;6:23770. doi: 10.1038/srep23770.


BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell.

Deeney JT, Belkina AC, Shirihai OS, Corkey BE, Denis GV.

PLoS One. 2016 Mar 23;11(3):e0151329. doi: 10.1371/journal.pone.0151329. eCollection 2016.


Characterizing the Covalent Targets of a Small Molecule Inhibitor of the Lysine Acetyltransferase P300.

Shrimp JH, Sorum AW, Garlick JM, Guasch L, Nicklaus MC, Meier JL.

ACS Med Chem Lett. 2015 Oct 31;7(2):151-5. doi: 10.1021/acsmedchemlett.5b00385. eCollection 2016 Feb 11.


Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.

Taylor AM, Vaswani RG, Gehling VS, Hewitt MC, Leblanc Y, Audia JE, Bellon S, Cummings RT, Côté A, Harmange JC, Jayaram H, Joshi S, Lora JM, Mertz JA, Neiss A, Pardo E, Nasveschuk CG, Poy F, Sandy P, Setser JW, Sims RJ 3rd, Tang Y, Albrecht BK.

ACS Med Chem Lett. 2015 Mar 25;7(2):145-50. doi: 10.1021/ml500411h. eCollection 2016 Feb 11.


Frapid: achieving full automation of FRAP for chemical probe validation.

Yapp C, Rogers C, Savitsky P, Philpott M, Müller S.

Biomed Opt Express. 2016 Jan 11;7(2):422-41. doi: 10.1364/BOE.7.000422. eCollection 2016 Feb 1.


High-throughput small molecule screen identifies inhibitors of aberrant chromatin accessibility.

Pattenden SG, Simon JM, Wali A, Jayakody CN, Troutman J, McFadden AW, Wooten J, Wood CC, Frye SV, Janzen WP, Davis IJ.

Proc Natl Acad Sci U S A. 2016 Mar 15;113(11):3018-23. doi: 10.1073/pnas.1521827113. Epub 2016 Feb 29.


MCM5 as a target of BET inhibitors in thyroid cancer cells.

Mio C, Lavarone E, Conzatti K, Baldan F, Toffoletto B, Puppin C, Filetti S, Durante C, Russo D, Orlacchio A, Di Cristofano A, Di Loreto C, Damante G.

Endocr Relat Cancer. 2016 Apr;23(4):335-47. doi: 10.1530/ERC-15-0322. Epub 2016 Feb 24.


The Bromodomain BET Inhibitor JQ1 Suppresses Tumor Angiogenesis in Models of Childhood Sarcoma.

Bid HK, Phelps DA, Xaio L, Guttridge DC, Lin J, London C, Baker LH, Mo X, Houghton PJ.

Mol Cancer Ther. 2016 May;15(5):1018-28. doi: 10.1158/1535-7163.MCT-15-0567. Epub 2016 Feb 23.


Structure of the Brd4 ET domain bound to a C-terminal motif from γ-retroviral integrases reveals a conserved mechanism of interaction.

Crowe BL, Larue RC, Yuan C, Hess S, Kvaratskhelia M, Foster MP.

Proc Natl Acad Sci U S A. 2016 Feb 23;113(8):2086-91. doi: 10.1073/pnas.1516813113. Epub 2016 Feb 8.


High level of BRD4 promotes non-small cell lung cancer progression.

Liao YF, Wu YB, Long X, Zhu SQ, Jin C, Xu JJ, Ding JY.

Oncotarget. 2016 Feb 23;7(8):9491-500. doi: 10.18632/oncotarget.7068.

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