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Items: 1 to 20 of 87

1.

Configuration of a high-content imaging platform for hit identification and pharmacological assessment of JMJD3 demethylase enzyme inhibitors.

Mulji A, Haslam C, Brown F, Randle R, Karamshi B, Smith J, Eagle R, Munoz-Muriedas J, Taylor J, Sheikh A, Bridges A, Gill K, Jepras R, Smee P, Barker M, Woodrow M, Liddle J, Thomas P, Jones E, Gordon L, Tanner R, Leveridge M, Hutchinson S, Martin M, Brown M, Kruidenier L, Katso R.

J Biomol Screen. 2012 Jan;17(1):108-20. doi: 10.1177/1087057111418229.

PMID:
22223398
2.

JMJD3 is a histone H3K27 demethylase.

Xiang Y, Zhu Z, Han G, Lin H, Xu L, Chen CD.

Cell Res. 2007 Oct;17(10):850-7.

3.

High-throughput TR-FRET assays for identifying inhibitors of LSD1 and JMJD2C histone lysine demethylases.

Yu V, Fisch T, Long AM, Tang J, Lee JH, Hierl M, Chen H, Yakowec P, Schwandner R, Emkey R.

J Biomol Screen. 2012 Jan;17(1):27-38. doi: 10.1177/1087057111418228. Epub 2011 Aug 21.

PMID:
21859682
4.

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM.

Nature. 2012 Aug 16;488(7411):404-8. doi: 10.1038/nature11262.

5.

The histone H3 Lys 27 demethylase JMJD3 regulates gene expression by impacting transcriptional elongation.

Chen S, Ma J, Wu F, Xiong LJ, Ma H, Xu W, Lv R, Li X, Villen J, Gygi SP, Liu XS, Shi Y.

Genes Dev. 2012 Jun 15;26(12):1364-75. doi: 10.1101/gad.186056.111.

6.

Enabling lead discovery for histone lysine demethylases by high-throughput RapidFire mass spectrometry.

Hutchinson SE, Leveridge MV, Heathcote ML, Francis P, Williams L, Gee M, Munoz-Muriedas J, Leavens B, Shillings A, Jones E, Homes P, Baddeley S, Chung CW, Bridges A, Argyrou A.

J Biomol Screen. 2012 Jan;17(1):39-48. doi: 10.1177/1087057111416660. Epub 2011 Aug 21.

PMID:
21859681
7.

Novel Scaffolds of Cell-Active Histone Demethylase Inhibitors Identified from High-Throughput Screening.

Wang W, Marholz LJ, Wang X.

J Biomol Screen. 2015 Jul;20(6):821-7. doi: 10.1177/1087057115579637. Epub 2015 Apr 16.

8.

The localization of histone H3K27me3 demethylase Jmjd3 is dynamically regulated.

Kamikawa YF, Donohoe ME.

Epigenetics. 2014 Jun;9(6):834-41. doi: 10.4161/epi.28524. Epub 2014 Mar 19.

9.

TR-FRET cellular assays for interrogating posttranslational modifications of histone H3.

Machleidt T, Robers MB, Hermanson SB, Dudek JM, Bi K.

J Biomol Screen. 2011 Dec;16(10):1236-46. doi: 10.1177/1087057111422943. Epub 2011 Oct 4.

PMID:
21972037
10.

Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C).

Leurs U, Clausen RP, Kristensen JL, Lohse B.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5811-3. doi: 10.1016/j.bmcl.2012.07.091. Epub 2012 Aug 2.

PMID:
22917519
11.

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
12.

Inhibited expression of hematopoietic progenitor kinase 1 associated with loss of jumonji domain containing 3 promoter binding contributes to autoimmunity in systemic lupus erythematosus.

Zhang Q, Long H, Liao J, Zhao M, Liang G, Wu X, Zhang P, Ding S, Luo S, Lu Q.

J Autoimmun. 2011 Nov;37(3):180-9. doi: 10.1016/j.jaut.2011.09.006. Epub 2011 Oct 19.

PMID:
22014533
13.

Development of homogeneous nonradioactive methyltransferase and demethylase assays targeting histone H3 lysine 4.

Gauthier N, Caron M, Pedro L, Arcand M, Blouin J, Labonté A, Normand C, Paquet V, Rodenbrock A, Roy M, Rouleau N, Beaudet L, Padrós J, Rodriguez-Suarez R.

J Biomol Screen. 2012 Jan;17(1):49-58. doi: 10.1177/1087057111416659. Epub 2011 Sep 21.

PMID:
21940714
14.

H3K27 Demethylase JMJD3 Employs the NF-κB and BMP Signaling Pathways to Modulate the Tumor Microenvironment and Promote Melanoma Progression and Metastasis.

Park WY, Hong BJ, Lee J, Choi C, Kim MY.

Cancer Res. 2016 Jan 1;76(1):161-70. doi: 10.1158/0008-5472.CAN-15-0536.

15.

Epigenetic regulation of osteoclast differentiation: possible involvement of Jmjd3 in the histone demethylation of Nfatc1.

Yasui T, Hirose J, Tsutsumi S, Nakamura K, Aburatani H, Tanaka S.

J Bone Miner Res. 2011 Nov;26(11):2665-71. doi: 10.1002/jbmr.464.

16.

A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening.

Wigle TJ, Swinger KK, Campbell JE, Scholle MD, Sherrill J, Admirand EA, Boriack-Sjodin PA, Kuntz KW, Chesworth R, Moyer MP, Scott MP, Copeland RA.

J Biomol Screen. 2015 Jul;20(6):810-20. doi: 10.1177/1087057115575689. Epub 2015 Mar 9.

PMID:
25755264
17.

Jmjd3-mediated epigenetic regulation of inflammatory cytokine gene expression in serum amyloid A-stimulated macrophages.

Yan Q, Sun L, Zhu Z, Wang L, Li S, Ye RD.

Cell Signal. 2014 Sep;26(9):1783-91. doi: 10.1016/j.cellsig.2014.03.025. Epub 2014 Apr 1.

18.

Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.

King ON, Li XS, Sakurai M, Kawamura A, Rose NR, Ng SS, Quinn AM, Rai G, Mott BT, Beswick P, Klose RJ, Oppermann U, Jadhav A, Heightman TD, Maloney DJ, Schofield CJ, Simeonov A.

PLoS One. 2010 Nov 23;5(11):e15535. doi: 10.1371/journal.pone.0015535.

19.

Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.

Hu J, Wang X, Chen L, Huang M, Tang W, Zuo J, Liu YC, Shi Z, Liu R, Shen J, Xiong B.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):721-725. doi: 10.1016/j.bmcl.2016.01.006. Epub 2016 Jan 7.

PMID:
26776360
20.

The future therapeutic potential of histone demethylases: A critical analysis.

Natoli G, Testa G, De Santa F.

Curr Opin Drug Discov Devel. 2009 Sep;12(5):607-15. Review.

PMID:
19736620

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