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Items: 1 to 20 of 157

1.

Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2.

Liu S, Walker SR, Nelson EA, Cerulli R, Xiang M, Toniolo PA, Qi J, Stone RM, Wadleigh M, Bradner JE, Frank DA.

Mol Cancer Ther. 2014 May;13(5):1194-205. doi: 10.1158/1535-7163.MCT-13-0341. Epub 2014 Jan 16.

2.

Inhibition of BET bromodomain targets genetically diverse glioblastoma.

Cheng Z, Gong Y, Ma Y, Lu K, Lu X, Pierce LA, Thompson RC, Muller S, Knapp S, Wang J.

Clin Cancer Res. 2013 Apr 1;19(7):1748-59. doi: 10.1158/1078-0432.CCR-12-3066. Epub 2013 Feb 12.

3.

Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer.

Shimamura T, Chen Z, Soucheray M, Carretero J, Kikuchi E, Tchaicha JH, Gao Y, Cheng KA, Cohoon TJ, Qi J, Akbay E, Kimmelman AC, Kung AL, Bradner JE, Wong KK.

Clin Cancer Res. 2013 Nov 15;19(22):6183-92. doi: 10.1158/1078-0432.CCR-12-3904. Epub 2013 Sep 17.

4.

BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism.

Boehm D, Calvanese V, Dar RD, Xing S, Schroeder S, Martins L, Aull K, Li PC, Planelles V, Bradner JE, Zhou MM, Siliciano RF, Weinberger L, Verdin E, Ott M.

Cell Cycle. 2013 Feb 1;12(3):452-62. doi: 10.4161/cc.23309. Epub 2012 Feb 1.

5.

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.

6.

BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.

Belkina AC, Nikolajczyk BS, Denis GV.

J Immunol. 2013 Apr 1;190(7):3670-8. doi: 10.4049/jimmunol.1202838. Epub 2013 Feb 18.

7.

Inhibiting STAT5 by the BET bromodomain inhibitor JQ1 disrupts human dendritic cell maturation.

Toniolo PA, Liu S, Yeh JE, Moraes-Vieira PM, Walker SR, Vafaizadeh V, Barbuto JA, Frank DA.

J Immunol. 2015 Apr 1;194(7):3180-90. doi: 10.4049/jimmunol.1401635. Epub 2015 Feb 27.

8.

Signal transducer and activator of transcription STAT5 is recruited to c-Myc super-enhancer.

Pinz S, Unser S, Rascle A.

BMC Mol Biol. 2016 Apr 14;17:10. doi: 10.1186/s12867-016-0063-y.

9.

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.

Ceribelli M, Kelly PN, Shaffer AL, Wright GW, Xiao W, Yang Y, Mathews Griner LA, Guha R, Shinn P, Keller JM, Liu D, Patel PR, Ferrer M, Joshi S, Nerle S, Sandy P, Normant E, Thomas CJ, Staudt LM.

Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):11365-70. doi: 10.1073/pnas.1411701111. Epub 2014 Jul 21.

10.

Deacetylase inhibitors repress STAT5-mediated transcription by interfering with bromodomain and extra-terminal (BET) protein function.

Pinz S, Unser S, Buob D, Fischer P, Jobst B, Rascle A.

Nucleic Acids Res. 2015 Apr 20;43(7):3524-45. doi: 10.1093/nar/gkv188. Epub 2015 Mar 13.

11.

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.

Stewart HJ, Horne GA, Bastow S, Chevassut TJ.

Cancer Med. 2013 Dec;2(6):826-35. doi: 10.1002/cam4.146. Epub 2013 Oct 31.

12.

Bromodomain inhibitors, JQ1 and I-BET 762, as potential therapies for pancreatic cancer.

Leal AS, Williams CR, Royce DB, Pioli PA, Sporn MB, Liby KT.

Cancer Lett. 2017 May 28;394:76-87. doi: 10.1016/j.canlet.2017.02.021. Epub 2017 Feb 27.

PMID:
28254412
13.

The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis.

Belkina AC, Blanton WP, Nikolajczyk BS, Denis GV.

J Leukoc Biol. 2014 Mar;95(3):451-60. doi: 10.1189/jlb.1112588. Epub 2013 Dec 6.

14.

Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors.

Tolani B, Gopalakrishnan R, Punj V, Matta H, Chaudhary PM.

Oncogene. 2014 May 29;33(22):2928-37. doi: 10.1038/onc.2013.242. Epub 2013 Jun 24.

15.

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.

16.

Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase-dependent NF-κB activation in rheumatoid fibroblast-like synoviocytes.

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

Rheumatology (Oxford). 2016 Jan;55(1):173-84. doi: 10.1093/rheumatology/kev312. Epub 2015 Aug 31.

PMID:
26324948
17.

Inhibition of the acetyl lysine-binding pocket of bromodomain and extraterminal domain proteins interferes with adipogenesis.

Goupille O, Penglong T, Kadri Z, Granger-Locatelli M, Fucharoen S, Maouche-Chrétien L, Prost S, Leboulch P, Chrétien S.

Biochem Biophys Res Commun. 2016 Apr 15;472(4):624-30. doi: 10.1016/j.bbrc.2016.03.013. Epub 2016 Mar 10.

PMID:
26972250
18.

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.

Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H.

Mol Cancer Ther. 2016 Nov;15(11):2563-2574. Epub 2016 Aug 29.

PMID:
27573426
19.

Sensitivity of Small Cell Lung Cancer to BET Inhibition Is Mediated by Regulation of ASCL1 Gene Expression.

Lenhart R, Kirov S, Desilva H, Cao J, Lei M, Johnston K, Peterson R, Schweizer L, Purandare A, Ross-Macdonald P, Fairchild C, Wong T, Wee S.

Mol Cancer Ther. 2015 Oct;14(10):2167-74. doi: 10.1158/1535-7163.MCT-15-0037. Epub 2015 Aug 7.

20.

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.

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