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Results: 1 to 20 of 111

1.

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, Stankovic T, Knapp S.

Cancer Res. 2013 Jun 1;73(11):3336-46. doi: 10.1158/0008-5472.CAN-12-3292. Epub 2013 Apr 10.

PMID:
23576556
[PubMed - indexed for MEDLINE]
Free PMC Article
2.

Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.

Jung M, Philpott M, Müller S, Schulze J, Badock V, Eberspächer U, Moosmayer D, Bader B, Schmees N, Fernández-Montalván A, Haendler B.

J Biol Chem. 2014 Mar 28;289(13):9304-19. doi: 10.1074/jbc.M113.523019. Epub 2014 Feb 4.

PMID:
24497639
[PubMed - indexed for MEDLINE]
Free PMC Article
3.

Targeting MYCN in neuroblastoma by BET bromodomain inhibition.

Puissant A, Frumm SM, Alexe G, Bassil CF, Qi J, Chanthery YH, Nekritz EA, Zeid R, Gustafson WC, Greninger P, Garnett MJ, McDermott U, Benes CH, Kung AL, Weiss WA, Bradner JE, Stegmaier K.

Cancer Discov. 2013 Mar;3(3):308-23. doi: 10.1158/2159-8290.CD-12-0418. Epub 2013 Feb 21.

PMID:
23430699
[PubMed - indexed for MEDLINE]
Free PMC Article
4.

Structures of the dual bromodomains of the P-TEFb-activating protein Brd4 at atomic resolution.

Vollmuth F, Blankenfeldt W, Geyer M.

J Biol Chem. 2009 Dec 25;284(52):36547-56. doi: 10.1074/jbc.M109.033712. Epub 2009 Oct 13.

PMID:
19828451
[PubMed - indexed for MEDLINE]
Free PMC Article
5.

Targeting MYC dependence in cancer by inhibiting BET bromodomains.

Mertz JA, Conery AR, Bryant BM, Sandy P, Balasubramanian S, Mele DA, Bergeron L, Sims RJ 3rd.

Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74. doi: 10.1073/pnas.1108190108. Epub 2011 Sep 26.

PMID:
21949397
[PubMed - indexed for MEDLINE]
Free PMC Article
6.

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ.

PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013.

PMID:
24009722
[PubMed - indexed for MEDLINE]
Free PMC Article
7.

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.

Mirguet O, Gosmini R, Toum J, Clément CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes AC, Smithers NN, Chung CW, Bamborough P, Uings IJ, Lewis A, Witherington J, Parr N, Prinjha RK, Nicodème E.

J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25.

PMID:
24015967
[PubMed - indexed for MEDLINE]
8.

Solution structure of the second bromodomain of Brd2 and its specific interaction with acetylated histone tails.

Huang H, Zhang J, Shen W, Wang X, Wu J, Wu J, Shi Y.

BMC Struct Biol. 2007 Sep 12;7:57.

PMID:
17848202
[PubMed - indexed for MEDLINE]
Free PMC Article
9.

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.

Ott CJ, Kopp N, Bird L, Paranal RM, Qi J, Bowman T, Rodig SJ, Kung AL, Bradner JE, Weinstock DM.

Blood. 2012 Oct 4;120(14):2843-52. doi: 10.1182/blood-2012-02-413021. Epub 2012 Aug 17.

PMID:
22904298
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

Selective inhibition of BET bromodomains.

Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE.

Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24.

PMID:
20871596
[PubMed - indexed for MEDLINE]
Free PMC Article
11.

Kaposi's sarcoma-associated herpesvirus LANA-1 interacts with the short variant of BRD4 and releases cells from a BRD4- and BRD2/RING3-induced G1 cell cycle arrest.

Ottinger M, Christalla T, Nathan K, Brinkmann MM, Viejo-Borbolla A, Schulz TF.

J Virol. 2006 Nov;80(21):10772-86. Epub 2006 Aug 23.

PMID:
16928766
[PubMed - indexed for MEDLINE]
Free PMC Article
12.

Structural basis and binding properties of the second bromodomain of Brd4 with acetylated histone tails.

Liu Y, Wang X, Zhang J, Huang H, Ding B, Wu J, Shi Y.

Biochemistry. 2008 Jun 17;47(24):6403-17. doi: 10.1021/bi8001659. Epub 2008 May 24.

PMID:
18500820
[PubMed - indexed for MEDLINE]
13.

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD.

J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8.

PMID:
23095041
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

When are the BET factors the most sensitive to bromodomain inhibitors?

Khochbin S.

Transcription. 2013 Mar-Apr;4(2):54-7. doi: 10.4161/trns.23191. Epub 2013 Feb 14.

PMID:
23412362
[PubMed - indexed for MEDLINE]
Free PMC Article
15.

Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins.

Lockwood WW, Zejnullahu K, Bradner JE, Varmus H.

Proc Natl Acad Sci U S A. 2012 Nov 20;109(47):19408-13. doi: 10.1073/pnas.1216363109. Epub 2012 Nov 5.

PMID:
23129625
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

BRD4 sustains melanoma proliferation and represents a new target for epigenetic therapy.

Segura MF, Fontanals-Cirera B, Gaziel-Sovran A, Guijarro MV, Hanniford D, Zhang G, González-Gomez P, Morante M, Jubierre L, Zhang W, Darvishian F, Ohlmeyer M, Osman I, Zhou MM, Hernando E.

Cancer Res. 2013 Oct 15;73(20):6264-76. doi: 10.1158/0008-5472.CAN-13-0122-T. Epub 2013 Aug 15.

PMID:
23950209
[PubMed - indexed for MEDLINE]
17.

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.

Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD.

J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6.

PMID:
21851057
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

The double bromodomain protein Brd4 binds to acetylated chromatin during interphase and mitosis.

Dey A, Chitsaz F, Abbasi A, Misteli T, Ozato K.

Proc Natl Acad Sci U S A. 2003 Jul 22;100(15):8758-63. Epub 2003 Jul 2.

PMID:
12840145
[PubMed - indexed for MEDLINE]
Free PMC Article
19.

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.

Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P.

Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18.

PMID:
24248379
[PubMed - indexed for MEDLINE]
Free PMC Article
20.

Bromodomains as therapeutic targets in cancer.

Barbieri I, Cannizzaro E, Dawson MA.

Brief Funct Genomics. 2013 May;12(3):219-30. doi: 10.1093/bfgp/elt007. Epub 2013 Mar 28. Review.

PMID:
23543289
[PubMed - indexed for MEDLINE]

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