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Items: 1 to 20 of 102

1.

Quantitative analysis of histone demethylase probes using fluorescence polarization.

Xu W, Podoll JD, Dong X, Tumber A, Oppermann U, Wang X.

J Med Chem. 2013 Jun 27;56(12):5198-202. doi: 10.1021/jm3018628. Epub 2013 Jun 13.

2.

Development of substrate-selective probes for affinity pulldown of histone demethylases.

Marholz LJ, Chang L, Old WM, Wang X.

ACS Chem Biol. 2015 Jan 16;10(1):129-37. doi: 10.1021/cb5006867. Epub 2014 Oct 29.

3.

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.

4.

A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

Luo X, Liu Y, Kubicek S, Myllyharju J, Tumber A, Ng S, Che KH, Podoll J, Heightman TD, Oppermann U, Schreiber SL, Wang X.

J Am Chem Soc. 2011 Jun 22;133(24):9451-6. doi: 10.1021/ja201597b. Epub 2011 May 31.

5.

Substrate- and cofactor-independent inhibition of histone demethylase KDM4C.

Leurs U, Lohse B, Rand KD, Ming S, Riise ES, Cole PA, Kristensen JL, Clausen RP.

ACS Chem Biol. 2014 Sep 19;9(9):2131-8. doi: 10.1021/cb500374f. Epub 2014 Jul 17.

6.

Targeting histone lysine demethylases by truncating the histone 3 tail to obtain selective substrate-based inhibitors.

Lohse B, Nielsen AL, Kristensen JB, Helgstrand C, Cloos PA, Olsen L, Gajhede M, Clausen RP, Kristensen JL.

Angew Chem Int Ed Engl. 2011 Sep 19;50(39):9100-3. doi: 10.1002/anie.201101849. Epub 2011 Aug 25. No abstract available.

PMID:
21919140
7.

A scintillation proximity assay for histone demethylases.

Yu W, Eram MS, Hajian T, Szykowska A, Burgess-Brown N, Vedadi M, Brown PJ.

Anal Biochem. 2014 Oct 15;463:54-60. doi: 10.1016/j.ab.2014.06.023. Epub 2014 Jul 8.

PMID:
25010373
8.

Recent Progress in Histone Demethylase Inhibitors.

McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ.

J Med Chem. 2016 Feb 25;59(4):1308-29. doi: 10.1021/acs.jmedchem.5b01758. Epub 2016 Feb 2. Review.

PMID:
26710088
9.

Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases.

Horton JR, Engstrom A, Zoeller EL, Liu X, Shanks JR, Zhang X, Johns MA, Vertino PM, Fu H, Cheng X.

J Biol Chem. 2016 Feb 5;291(6):2631-46. doi: 10.1074/jbc.M115.698449. Epub 2015 Dec 8.

10.

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
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.

Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity.

Schmitt ML, Hauser AT, Carlino L, Pippel M, Schulz-Fincke J, Metzger E, Willmann D, Yiu T, Barton M, Schüle R, Sippl W, Jung M.

J Med Chem. 2013 Sep 26;56(18):7334-42. doi: 10.1021/jm400792m. Epub 2013 Sep 5.

13.

Histone H3 peptide based LSD1-selective inhibitors.

Kakizawa T, Ota Y, Itoh Y, Tsumoto H, Suzuki T.

Bioorg Med Chem Lett. 2015 May 1;25(9):1925-8. doi: 10.1016/j.bmcl.2015.03.030. Epub 2015 Mar 20.

PMID:
25827526
14.

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
15.

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
16.

Compounds and methods for inhibiting histone demethylases: a patent evaluation of US20160102096A1.

Thaler F, Mercurio C.

Expert Opin Ther Pat. 2016 Dec;26(12):1367-1370. Epub 2016 Oct 21.

PMID:
27730846
17.

The role of histone demethylases in cancer therapy.

Hoffmann I, Roatsch M, Schmitt ML, Carlino L, Pippel M, Sippl W, Jung M.

Mol Oncol. 2012 Dec;6(6):683-703. doi: 10.1016/j.molonc.2012.07.004. Epub 2012 Aug 7. Review.

18.

Azalysine analogues as probes for protein lysine deacetylation and demethylation.

Dancy BC, Ming SA, Papazyan R, Jelinek CA, Majumdar A, Sun Y, Dancy BM, Drury WJ 3rd, Cotter RJ, Taverna SD, Cole PA.

J Am Chem Soc. 2012 Mar 21;134(11):5138-48. doi: 10.1021/ja209574z. Epub 2012 Mar 12.

19.

A sensitive, homogeneous, and high-throughput assay for lysine-specific histone demethylases at the H3K4 site.

Wang C, Caron M, Burdick D, Kang Z, Auld D, Hill WA, Padrós J, Zhang JH.

Assay Drug Dev Technol. 2012 Apr;10(2):179-86. doi: 10.1089/adt.2011.0395. Epub 2011 Dec 22.

PMID:
22192306
20.

An ultra-high throughput screening approach for an adenine transferase using fluorescence polarization.

Li Z, Mehdi S, Patel I, Kawooya J, Judkins M, Zhang W, Diener K, Lozada A, Dunnington D.

J Biomol Screen. 2000 Feb;5(1):31-8.

PMID:
10841598

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