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Items: 1 to 50 of 87

1.

Targeting enhancer switching overcomes non-genetic drug resistance in acute myeloid leukaemia.

Bell CC, Fennell KA, Chan YC, Rambow F, Yeung MM, Vassiliadis D, Lara L, Yeh P, Martelotto LG, Rogiers A, Kremer BE, Barbash O, Mohammad HP, Johanson TM, Burr ML, Dhar A, Karpinich N, Tian L, Tyler DS, MacPherson L, Shi J, Pinnawala N, Yew Fong C, Papenfuss AT, Grimmond SM, Dawson SJ, Allan RS, Kruger RG, Vakoc CR, Goode DL, Naik SH, Gilan O, Lam EYN, Marine JC, Prinjha RK, Dawson MA.

Nat Commun. 2019 Jun 20;10(1):2723. doi: 10.1038/s41467-019-10652-9.

PMID:
31222014
2.

Bromodomain inhibitor I-BET151 suppresses immune responses during fungal-immune interaction.

Domínguez-Andrés J, Ferreira AV, Jansen T, Smithers N, Prinjha RK, Furze RC, Netea MG.

Eur J Immunol. 2019 Jun 17. doi: 10.1002/eji.201848081. [Epub ahead of print]

PMID:
31206650
3.

Advancements in the Development of non-BET Bromodomain Chemical Probes.

Clegg MA, Tomkinson NCO, Prinjha RK, Humphreys PG.

ChemMedChem. 2019 Feb 19;14(4):362-385. doi: 10.1002/cmdc.201800738. Epub 2019 Feb 4. Review.

PMID:
30624862
4.

SRPK1 maintains acute myeloid leukemia through effects on isoform usage of epigenetic regulators including BRD4.

Tzelepis K, De Braekeleer E, Aspris D, Barbieri I, Vijayabaskar MS, Liu WH, Gozdecka M, Metzakopian E, Toop HD, Dudek M, Robson SC, Hermida-Prado F, Yang YH, Babaei-Jadidi R, Garyfallos DA, Ponstingl H, Dias JML, Gallipoli P, Seiler M, Buonamici S, Vick B, Bannister AJ, Rad R, Prinjha RK, Marioni JC, Huntly B, Batson J, Morris JC, Pina C, Bradley A, Jeremias I, Bates DO, Yusa K, Kouzarides T, Vassiliou GS.

Nat Commun. 2018 Dec 19;9(1):5378. doi: 10.1038/s41467-018-07620-0.

5.

Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-trans retinoic acid in acute myeloid leukemia across subtypes.

Smitheman KN, Severson TM, Rajapurkar SR, McCabe MT, Karpinich N, Foley J, Pappalardi MB, Hughes A, Halsey W, Thomas E, Traini C, Federowicz KE, Laraio J, Mobegi F, Ferron-Brady G, Prinjha RK, Carpenter CL, Kruger RG, Wessels L, Mohammad HP.

Haematologica. 2019 Jun;104(6):1156-1167. doi: 10.3324/haematol.2018.199190. Epub 2018 Dec 4.

6.

BET Inhibition Improves NASH and Liver Fibrosis.

Middleton SA, Rajpal N, Cutler L, Mander P, Rioja I, Prinjha RK, Rajpal D, Agarwal P, Kumar V.

Sci Rep. 2018 Nov 22;8(1):17257. doi: 10.1038/s41598-018-35653-4.

7.

Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.

Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Watson RJ, Mitchell DJ, Barnett H, Prinjha RK, Rau C, Sheppard RJ, Werner T, Demont EH.

J Med Chem. 2018 Sep 27;61(18):8321-8336. doi: 10.1021/acs.jmedchem.8b00862. Epub 2018 Sep 18.

PMID:
30226378
8.

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

Bassi ZI, Fillmore MC, Miah AH, Chapman TD, Maller C, Roberts EJ, Davis LC, Lewis DE, Galwey NW, Waddington KE, Parravicini V, Macmillan-Jones AL, Gongora C, Humphreys PG, Churcher I, Prinjha RK, Tough DF.

ACS Chem Biol. 2018 Oct 19;13(10):2862-2867. doi: 10.1021/acschembio.8b00705. Epub 2018 Sep 18.

PMID:
30200762
9.

Influenza virus infection causes global RNAPII termination defects.

Zhao N, Sebastiano V, Moshkina N, Mena N, Hultquist J, Jimenez-Morales D, Ma Y, Rialdi A, Albrecht R, Fenouil R, Sánchez-Aparicio MT, Ayllon J, Ravisankar S, Haddad B, Ho JSY, Low D, Jin J, Yurchenko V, Prinjha RK, Tarakhovsky A, Squatrito M, Pinto D, Allette K, Byun M, Smith ML, Sebra R, Guccione E, Tumpey T, Krogan N, Greenbaum B, van Bakel H, García-Sastre A, Marazzi I.

Nat Struct Mol Biol. 2018 Sep;25(9):885-893. doi: 10.1038/s41594-018-0124-7. Epub 2018 Sep 3.

PMID:
30177761
10.

Inhibition of BET Proteins Reduces Right Ventricle Hypertrophy and Pulmonary Hypertension Resulting from Combined Hypoxia and Pulmonary Inflammation.

Chabert C, Khochbin S, Rousseaux S, Veyrenc S, Furze R, Smithers N, Prinjha RK, Schlattner U, Pison C, Dubouchaud H.

Int J Mol Sci. 2018 Jul 30;19(8). pii: E2224. doi: 10.3390/ijms19082224.

11.

Drawing on disorder: How viruses use histone mimicry to their advantage.

Tarakhovsky A, Prinjha RK.

J Exp Med. 2018 Jul 2;215(7):1777-1787. doi: 10.1084/jem.20180099. Epub 2018 Jun 22. Review.

12.

Antileukemic Efficacy of BET Inhibitor in a Preclinical Mouse Model of MLL-AF4+ Infant ALL.

Bardini M, Trentin L, Rizzo F, Vieri M, Savino AM, Garrido Castro P, Fazio G, Van Roon EHJ, Kerstjens M, Smithers N, Prinjha RK, Te Kronnie G, Basso G, Stam RW, Pieters R, Biondi A, Cazzaniga G.

Mol Cancer Ther. 2018 Aug;17(8):1705-1716. doi: 10.1158/1535-7163.MCT-17-1123. Epub 2018 May 10.

PMID:
29748211
13.

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.

Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.

J Med Chem. 2018 May 24;61(10):4317-4334. doi: 10.1021/acs.jmedchem.7b01666. Epub 2018 May 3.

PMID:
29656650
14.

BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.

Morse MA, Balogh KK, Brendle SA, Campbell CA, Chen MX, Furze RC, Harada IL, Holyer ID, Kumar U, Lee K, Prinjha RK, Rüdiger M, Seal JT, Taylor S, Witherington J, Christensen ND.

Antiviral Res. 2018 Jun;154:158-165. doi: 10.1016/j.antiviral.2018.03.012. Epub 2018 Apr 11.

15.

Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis.

Savitski MM, Zinn N, Faelth-Savitski M, Poeckel D, Gade S, Becher I, Muelbaier M, Wagner AJ, Strohmer K, Werner T, Melchert S, Petretich M, Rutkowska A, Vappiani J, Franken H, Steidel M, Sweetman GM, Gilan O, Lam EYN, Dawson MA, Prinjha RK, Grandi P, Bergamini G, Bantscheff M.

Cell. 2018 Mar 22;173(1):260-274.e25. doi: 10.1016/j.cell.2018.02.030. Epub 2018 Mar 15.

16.

Signaling function of PRC2 is essential for TCR-driven T cell responses.

Dobenecker MW, Park JS, Marcello J, McCabe MT, Gregory R, Knight SD, Rioja I, Bassil AK, Prinjha RK, Tarakhovsky A.

J Exp Med. 2018 Apr 2;215(4):1101-1113. doi: 10.1084/jem.20170084. Epub 2018 Mar 9.

17.

Ezh2 and Runx1 Mutations Collaborate to Initiate Lympho-Myeloid Leukemia in Early Thymic Progenitors.

Booth CAG, Barkas N, Neo WH, Boukarabila H, Soilleux EJ, Giotopoulos G, Farnoud N, Giustacchini A, Ashley N, Carrelha J, Jamieson L, Atkinson D, Bouriez-Jones T, Prinjha RK, Milne TA, Teachey DT, Papaemmanuil E, Huntly BJP, Jacobsen SEW, Mead AJ.

Cancer Cell. 2018 Feb 12;33(2):274-291.e8. doi: 10.1016/j.ccell.2018.01.006.

18.

Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.

Cribbs A, Hookway ES, Wells G, Lindow M, Obad S, Oerum H, Prinjha RK, Athanasou N, Sowman A, Philpott M, Penn H, Soderstrom K, Feldmann M, Oppermann U.

J Biol Chem. 2018 Feb 16;293(7):2422-2437. doi: 10.1074/jbc.RA117.000698. Epub 2018 Jan 4.

19.

Small molecules and their role in effective preclinical target validation.

Clegg MA, Tomkinson NC, Prinjha RK, Humphreys PG.

Future Med Chem. 2017 Sep;9(14):1579-1582. doi: 10.4155/fmc-2017-0121. Epub 2017 Aug 22. No abstract available.

20.

Selective inhibition of BET proteins reduces pancreatic damage and systemic inflammation in bile acid- and fatty acid ethyl ester- but not caerulein-induced acute pancreatitis.

Huang W, Haynes AC, Mukherjee R, Wen L, Latawiec D, Tepikin AV, Criddle DN, Prinjha RK, Smithers N, Sutton R.

Pancreatology. 2017 Sep - Oct;17(5):689-697. doi: 10.1016/j.pan.2017.06.005. Epub 2017 Jun 10.

PMID:
28648518
21.

Click chemistry enables preclinical evaluation of targeted epigenetic therapies.

Tyler DS, Vappiani J, Cañeque T, Lam EYN, Ward A, Gilan O, Chan YC, Hienzsch A, Rutkowska A, Werner T, Wagner AJ, Lugo D, Gregory R, Ramirez Molina C, Garton N, Wellaway CR, Jackson S, MacPherson L, Figueiredo M, Stolzenburg S, Bell CC, House C, Dawson SJ, Hawkins ED, Drewes G, Prinjha RK, Rodriguez R, Grandi P, Dawson MA.

Science. 2017 Jun 30;356(6345):1397-1401. doi: 10.1126/science.aal2066. Epub 2017 Jun 15.

22.

Assessing histone demethylase inhibitors in cells: lessons learned.

Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S.

Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017.

23.

Protein arginine deiminase 4 inhibition is sufficient for the amelioration of collagen-induced arthritis.

Willis VC, Banda NK, Cordova KN, Chandra PE, Robinson WH, Cooper DC, Lugo D, Mehta G, Taylor S, Tak PP, Prinjha RK, Lewis HD, Holers VM.

Clin Exp Immunol. 2017 May;188(2):263-274. doi: 10.1111/cei.12932. Epub 2017 Mar 9.

24.

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.

Humphreys PG, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Hayhow TG, Hussain J, Jones KL, Lindon M, Michon AM, Renaux JF, Suckling CJ, Tough DF, Prinjha RK.

J Med Chem. 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566. Epub 2017 Jan 9.

PMID:
28002667
25.

Immune disease-associated variants in gene enhancers point to BET epigenetic mechanisms for therapeutic intervention.

Tough DF, Prinjha RK.

Epigenomics. 2017 Apr;9(4):573-584. doi: 10.2217/epi-2016-0144. Epub 2016 Dec 7. Review.

26.

Epigenetic drug discovery: breaking through the immune barrier.

Tough DF, Tak PP, Tarakhovsky A, Prinjha RK.

Nat Rev Drug Discov. 2016 Dec;15(12):835-853. doi: 10.1038/nrd.2016.185. Epub 2016 Oct 21. Review.

PMID:
27765940
27.

BET bromodomain inhibition reduces maturation and enhances tolerogenic properties of human and mouse dendritic cells.

Schilderink R, Bell M, Reginato E, Patten C, Rioja I, Hilbers FW, Kabala PA, Reedquist KA, Tough DF, Tak PP, Prinjha RK, de Jonge WJ.

Mol Immunol. 2016 Nov;79:66-76. doi: 10.1016/j.molimm.2016.09.010. Epub 2016 Oct 3.

28.

A Chemical Probe for the ATAD2 Bromodomain.

Bamborough P, Chung CW, Demont EH, Furze RC, Bannister AJ, Che KH, Diallo H, Douault C, Grandi P, Kouzarides T, Michon AM, Mitchell DJ, Prinjha RK, Rau C, Robson S, Sheppard RJ, Upton R, Watson RJ.

Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6. doi: 10.1002/anie.201603928. Epub 2016 Aug 17.

PMID:
27530368
29.

Systematic chemical and molecular profiling of MLL-rearranged infant acute lymphoblastic leukemia reveals efficacy of romidepsin.

Cruickshank MN, Ford J, Cheung LC, Heng J, Singh S, Wells J, Failes TW, Arndt GM, Smithers N, Prinjha RK, Anderson D, Carter KW, Gout AM, Lassmann T, O'Reilly J, Cole CH, Kotecha RS, Kees UR.

Leukemia. 2017 Jan;31(1):40-50. doi: 10.1038/leu.2016.165. Epub 2016 Jun 13.

30.

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.

31.

Clinical progress and pharmacology of small molecule bromodomain inhibitors.

Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG.

Curr Opin Chem Biol. 2016 Aug;33:58-66. doi: 10.1016/j.cbpa.2016.05.028. Epub 2016 Jun 10. Review.

32.

Functional interdependence of BRD4 and DOT1L in MLL leukemia.

Gilan O, Lam EY, Becher I, Lugo D, Cannizzaro E, Joberty G, Ward A, Wiese M, Fong CY, Ftouni S, Tyler D, Stanley K, MacPherson L, Weng CF, Chan YC, Ghisi M, Smil D, Carpenter C, Brown P, Garton N, Blewitt ME, Bannister AJ, Kouzarides T, Huntly BJ, Johnstone RW, Drewes G, Dawson SJ, Arrowsmith CH, Grandi P, Prinjha RK, Dawson MA.

Nat Struct Mol Biol. 2016 Jul;23(7):673-81. doi: 10.1038/nsmb.3249. Epub 2016 Jun 13.

PMID:
27294782
33.

Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics.

Joberty G, Boesche M, Brown JA, Eberhard D, Garton NS, Humphreys PG, Mathieson T, Muelbaier M, Ramsden NG, Reader V, Rueger A, Sheppard RJ, Westaway SM, Bantscheff M, Lee K, Wilson DM, Prinjha RK, Drewes G.

ACS Chem Biol. 2016 Jul 15;11(7):2002-10. doi: 10.1021/acschembio.6b00080. Epub 2016 May 19.

PMID:
27197014
34.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.

Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK.

J Med Chem. 2016 Feb 25;59(4):1370-87. doi: 10.1021/acs.jmedchem.5b01538. Epub 2016 Jan 15.

PMID:
26771203
35.

Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.

Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK.

J Med Chem. 2016 Feb 25;59(4):1357-69. doi: 10.1021/acs.jmedchem.5b01537. Epub 2016 Jan 15.

PMID:
26771107
36.

Progress in the Development of non-BET Bromodomain Chemical Probes.

Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG.

ChemMedChem. 2016 Mar 4;11(5):477-87. doi: 10.1002/cmdc.201500540. Epub 2016 Jan 8. Review.

37.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.

Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J.

J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7.

38.

Bromodomain Proteins Contribute to Maintenance of Bloodstream Form Stage Identity in the African Trypanosome.

Schulz D, Mugnier MR, Paulsen EM, Kim HS, Chung CW, Tough DF, Rioja I, Prinjha RK, Papavasiliou FN, Debler EW.

PLoS Biol. 2015 Dec 8;13(12):e1002316. doi: 10.1371/journal.pbio.1002316. eCollection 2015 Dec.

39.

Epigenetic mechanisms and drug discovery in rheumatology.

Tough DF, Prinjha RK, Tak PP.

Clin Med (Lond). 2015 Dec;15 Suppl 6:s64-71. doi: 10.7861/clinmedicine.15-6-s64. Review.

PMID:
26634685
40.

Autism-like syndrome is induced by pharmacological suppression of BET proteins in young mice.

Sullivan JM, Badimon A, Schaefer U, Ayata P, Gray J, Chung CW, von Schimmelmann M, Zhang F, Garton N, Smithers N, Lewis H, Tarakhovsky A, Prinjha RK, Schaefer A.

J Exp Med. 2015 Oct 19;212(11):1771-81. doi: 10.1084/jem.20151271. Epub 2015 Sep 21.

41.

BET inhibitor resistance emerges from leukaemia stem cells.

Fong CY, Gilan O, Lam EY, Rubin AF, Ftouni S, Tyler D, Stanley K, Sinha D, Yeh P, Morison J, Giotopoulos G, Lugo D, Jeffrey P, Lee SC, Carpenter C, Gregory R, Ramsay RG, Lane SW, Abdel-Wahab O, Kouzarides T, Johnstone RW, Dawson SJ, Huntly BJ, Prinjha RK, Papenfuss AT, Dawson MA.

Nature. 2015 Sep 24;525(7570):538-42. doi: 10.1038/nature14888. Epub 2015 Sep 14.

42.

A novel mouse model identifies cooperating mutations and therapeutic targets critical for chronic myeloid leukemia progression.

Giotopoulos G, van der Weyden L, Osaki H, Rust AG, Gallipoli P, Meduri E, Horton SJ, Chan WI, Foster D, Prinjha RK, Pimanda JE, Tenen DG, Vassiliou GS, Koschmieder S, Adams DJ, Huntly BJ.

J Exp Med. 2015 Sep 21;212(10):1551-69. doi: 10.1084/jem.20141661. Epub 2015 Aug 24.

43.

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.

Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH.

J Med Chem. 2015 Aug 13;58(15):6151-78. doi: 10.1021/acs.jmedchem.5b00773. Epub 2015 Jul 31.

PMID:
26230603
44.

Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cells.

Yoshida H, Bansal K, Schaefer U, Chapman T, Rioja I, Proekt I, Anderson MS, Prinjha RK, Tarakhovsky A, Benoist C, Mathis D.

Proc Natl Acad Sci U S A. 2015 Aug 11;112(32):E4448-57. doi: 10.1073/pnas.1512081112. Epub 2015 Jul 27.

45.

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.

Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, Dixon DP, Douault C, Emmons AJ, Jones EJ, Karamshi BV, Locke K, Mitchell DJ, Mouzon BH, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ, Bamborough P.

J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9.

PMID:
26155854
46.

Combining BET and HDAC inhibitors synergistically induces apoptosis of melanoma and suppresses AKT and YAP signaling.

Heinemann A, Cullinane C, De Paoli-Iseppi R, Wilmott JS, Gunatilake D, Madore J, Strbenac D, Yang JY, Gowrishankar K, Tiffen JC, Prinjha RK, Smithers N, McArthur GA, Hersey P, Gallagher SJ.

Oncotarget. 2015 Aug 28;6(25):21507-21.

47.

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.

Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG.

J Med Chem. 2016 Feb 25;59(4):1425-39. doi: 10.1021/acs.jmedchem.5b00256. Epub 2015 Apr 30.

48.

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation.

Lewis HD, Liddle J, Coote JE, Atkinson SJ, Barker MD, Bax BD, Bicker KL, Bingham RP, Campbell M, Chen YH, Chung CW, Craggs PD, Davis RP, Eberhard D, Joberty G, Lind KE, Locke K, Maller C, Martinod K, Patten C, Polyakova O, Rise CE, Rüdiger M, Sheppard RJ, Slade DJ, Thomas P, Thorpe J, Yao G, Drewes G, Wagner DD, Thompson PR, Prinjha RK, Wilson DM.

Nat Chem Biol. 2015 Mar;11(3):189-91. doi: 10.1038/nchembio.1735. Epub 2015 Jan 26.

49.

The bromodomain protein inhibitor I-BET151 suppresses expression of inflammatory genes and matrix degrading enzymes in rheumatoid arthritis synovial fibroblasts.

Klein K, Kabala PA, Grabiec AM, Gay RE, Kolling C, Lin LL, Gay S, Tak PP, Prinjha RK, Ospelt C, Reedquist KA.

Ann Rheum Dis. 2016 Feb;75(2):422-9. doi: 10.1136/annrheumdis-2014-205809. Epub 2014 Dec 2.

PMID:
25467295
50.

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.

Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ.

ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13.

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