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Items: 25

1.

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.

2.

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.

3.

BET bromodomain inhibition promotes neurogenesis while inhibiting gliogenesis in neural progenitor cells.

Li J, Ma J, Meng G, Lin H, Wu S, Wang J, Luo J, Xu X, Tough D, Lindon M, Rioja I, Zhao J, Mei H, Prinjha R, Zhong Z.

Stem Cell Res. 2016 Sep;17(2):212-221. doi: 10.1016/j.scr.2016.07.006. Epub 2016 Jul 20.

4.

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.

5.

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
6.

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
7.

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.

8.

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.

9.

Epigenetic modulation of type-1 diabetes via a dual effect on pancreatic macrophages and β cells.

Fu W, Farache J, Clardy SM, Hattori K, Mander P, Lee K, Rioja I, Weissleder R, Prinjha RK, Benoist C, Mathis D.

Elife. 2014 Nov 19;3:e04631. doi: 10.7554/eLife.04631.

10.

Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.

Tough DF, Lewis HD, Rioja I, Lindon MJ, Prinjha RK.

Br J Pharmacol. 2014 Nov;171(22):4981-5010. doi: 10.1111/bph.12848. Review.

11.

BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms.

Wyspiańska BS, Bannister AJ, Barbieri I, Nangalia J, Godfrey A, Calero-Nieto FJ, Robson S, Rioja I, Li J, Wiese M, Cannizzaro E, Dawson MA, Huntly B, Prinjha RK, Green AR, Gottgens B, Kouzarides T.

Leukemia. 2014 Jan;28(1):88-97. doi: 10.1038/leu.2013.234. Epub 2013 Aug 9.

PMID:
23929215
12.

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24.

PMID:
22437115
13.

Histone H3 lysine 9 di-methylation as an epigenetic signature of the interferon response.

Fang TC, Schaefer U, Mecklenbrauker I, Stienen A, Dewell S, Chen MS, Rioja I, Parravicini V, Prinjha RK, Chandwani R, MacDonald MR, Lee K, Rice CM, Tarakhovsky A.

J Exp Med. 2012 Apr 9;209(4):661-9. doi: 10.1084/jem.20112343. Epub 2012 Mar 12.

14.

Quantitative power Doppler ultrasonography is a sensitive measure of metacarpophalangeal joint synovial vascularity in rheumatoid arthritis and declines significantly following a 2-week course of oral low-dose corticosteroids.

Larché MJ, Seymour M, Lim A, Eckersley RJ, Pétavy F, Chiesa F, Rioja I, Lukey PT, Binks M, McClinton C, Dolan K, Taylor PC.

J Rheumatol. 2010 Dec;37(12):2493-501. doi: 10.3899/jrheum.100322. Epub 2010 Oct 1.

PMID:
20889600
15.

In vitro target validation and in vivo efficacy of p38 MAP kinase inhibition in established chronic collagen-induced arthritis model: a pre-clinical study.

Triantaphyllopoulos K, Madden L, Rioja I, Essex D, Buckton J, Malhotra R, Ray K, Binks M, Paleolog EM.

Clin Exp Rheumatol. 2010 Mar-Apr;28(2):176-85. Epub 2010 May 13.

PMID:
20406612
16.

Potential novel biomarkers of disease activity in rheumatoid arthritis patients: CXCL13, CCL23, transforming growth factor alpha, tumor necrosis factor receptor superfamily member 9, and macrophage colony-stimulating factor.

Rioja I, Hughes FJ, Sharp CH, Warnock LC, Montgomery DS, Akil M, Wilson AG, Binks MH, Dickson MC.

Arthritis Rheum. 2008 Aug;58(8):2257-67. doi: 10.1002/art.23667.

17.

Gene expression profiles in the rat streptococcal cell wall-induced arthritis model identified using microarray analysis.

Rioja I, Clayton CL, Graham SJ, Life PF, Dickson MC.

Arthritis Res Ther. 2005;7(1):R101-17. Epub 2004 Nov 19.

18.
20.

A new ditriazine inhibitor of NF-kappaB modulates chronic inflammation and angiogenesis.

Rioja I, Terencio MC, Ubeda A, Riguera R, Quintela JM, Alcaraz MJ.

Naunyn Schmiedebergs Arch Pharmacol. 2002 May;365(5):357-64. Epub 2002 Mar 19.

PMID:
12012021
21.

A pyrroloquinazoline derivative with anti-inflammatory and analgesic activity by dual inhibition of cyclo-oxygenase-2 and 5-lipoxygenase.

Rioja I, Terencio MC, Ubeda A, Molina P, Tárraga A, Gonzalez-Tejero A, Alcaraz MJ.

Eur J Pharmacol. 2002 Jan 11;434(3):177-85.

PMID:
11779581
22.

Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.

Molina P, Tárraga A, Gonzalez-Tejero A, Rioja I, Ubeda A, Terencio MC, Alcaraz MJ.

J Nat Prod. 2001 Oct;64(10):1297-300.

PMID:
11678654
23.

Solid-phase synthesis and inhibitory effects of some pyrido[1,2-c]pyrimidine derivatives on leukocyte formations and experimental inflammation.

Molina P, Aller E, Lorenzo A, López-Cremades P, Rioja I, Ubeda A, Terencio MC, Alcaraz MJ.

J Med Chem. 2001 Mar 15;44(6):1011-4.

PMID:
11300882
24.

An anti-inflammatory ditriazine inhibiting leukocyte functions and expression of inducible nitric oxide synthase and cyclo-oxygenase-2.

Rioja I, Ubeda A, Terencio MC, Guillén I, Riguera R, Quintela JM, Peinador C, González LM, Alcaraz MJ.

Eur J Pharmacol. 2000 May 26;397(1):207-17.

PMID:
10844115
25.

Synthesis and pharmacological evaluation of some 8-cyanopyrido[3', 2':4,5]thieno[3,2-d]triazine derivatives as inhibitors of nitric oxide and eicosanoid biosynthesis.

Quintela JM, Peinador C, González LM, Riguera R, Rioja I, Terencio MC, Ubeda A, Alcaraz MJ.

J Med Chem. 1999 Nov 4;42(22):4720-4.

PMID:
10579834

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