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Items: 1 to 20 of 95

1.

Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.

Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N.

J Med Chem. 2013 Sep 26;56(18):7222-31. doi: 10.1021/jm400624b. Epub 2013 Sep 5.

2.

Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.

Hamada S, Suzuki T, Mino K, Koseki K, Oehme F, Flamme I, Ozasa H, Itoh Y, Ogasawara D, Komaarashi H, Kato A, Tsumoto H, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N.

J Med Chem. 2010 Aug 12;53(15):5629-38. doi: 10.1021/jm1003655.

PMID:
20684604
3.

Identification of cell-active lysine specific demethylase 1-selective inhibitors.

Ueda R, Suzuki T, Mino K, Tsumoto H, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N.

J Am Chem Soc. 2009 Dec 9;131(48):17536-7. doi: 10.1021/ja907055q.

PMID:
19950987
4.

Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors.

Benelkebir H, Hodgkinson C, Duriez PJ, Hayden AL, Bulleid RA, Crabb SJ, Packham G, Ganesan A.

Bioorg Med Chem. 2011 Jun 15;19(12):3709-16. doi: 10.1016/j.bmc.2011.02.017. Epub 2011 Feb 13.

PMID:
21382717
5.

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
6.

Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.

Zheng YC, Duan YC, Ma JL, Xu RM, Zi X, Lv WL, Wang MM, Ye XW, Zhu S, Mobley D, Zhu YY, Wang JW, Li JF, Wang ZR, Zhao W, Liu HM.

J Med Chem. 2013 Nov 14;56(21):8543-60. doi: 10.1021/jm401002r. Epub 2013 Nov 1.

7.

Structural analysis of human KDM5B guides histone demethylase inhibitor development.

Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U.

Nat Chem Biol. 2016 Jul;12(7):539-45. doi: 10.1038/nchembio.2087. Epub 2016 May 23.

PMID:
27214403
8.

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Rotili D, Tomassi S, Conte M, Benedetti R, Tortorici M, Ciossani G, Valente S, Marrocco B, Labella D, Novellino E, Mattevi A, Altucci L, Tumber A, Yapp C, King ON, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A.

J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802. Epub 2013 Dec 19.

PMID:
24325601
9.

Design, synthesis, and structure-activity relationship of novel LSD1 inhibitors based on pyrimidine-thiourea hybrids as potent, orally active antitumor agents.

Ma LY, Zheng YC, Wang SQ, Wang B, Wang ZR, Pang LP, Zhang M, Wang JW, Ding L, Li J, Wang C, Hu B, Liu Y, Zhang XD, Wang JJ, Wang ZJ, Zhao W, Liu HM.

J Med Chem. 2015 Feb 26;58(4):1705-16. doi: 10.1021/acs.jmedchem.5b00037. Epub 2015 Feb 6.

PMID:
25610955
10.

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A.

J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11.

11.

3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.

Wu F, Zhou C, Yao Y, Wei L, Feng Z, Deng L, Song Y.

J Med Chem. 2016 Jan 14;59(1):253-63. doi: 10.1021/acs.jmedchem.5b01361. Epub 2015 Dec 24.

12.

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.

13.

Synthesis and evaluation of 3-amino/guanidine substituted phenyl oxazoles as a novel class of LSD1 inhibitors with anti-proliferative properties.

Dulla B, Kirla KT, Rathore V, Deora GS, Kavela S, Maddika S, Chatti K, Reiser O, Iqbal J, Pal M.

Org Biomol Chem. 2013 May 21;11(19):3103-7. doi: 10.1039/c3ob40217g. Epub 2013 Apr 10.

PMID:
23575971
14.

The re-expression of the epigenetically silenced e-cadherin gene by a polyamine analogue lysine-specific demethylase-1 (LSD1) inhibitor in human acute myeloid leukemia cell lines.

Murray-Stewart T, Woster PM, Casero RA Jr.

Amino Acids. 2014 Mar;46(3):585-94. doi: 10.1007/s00726-013-1485-1. Epub 2013 Mar 19.

15.

Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence.

Hanessian S, Auzzas L, Giannini G, Marzi M, Cabri W, Barbarino M, Vesci L, Pisano C.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6261-5. Epub 2007 Sep 8.

PMID:
17892933
16.

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.

17.

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
18.

Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism.

Ogasawara D, Itoh Y, Tsumoto H, Kakizawa T, Mino K, Fukuhara K, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N, Suzuki T.

Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8620-4. doi: 10.1002/anie.201303999. Epub 2013 Jul 3. No abstract available.

PMID:
23824985
19.

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
20.

High-throughput virtual screening identifies novel N'-(1-phenylethylidene)-benzohydrazides as potent, specific, and reversible LSD1 inhibitors.

Sorna V, Theisen ER, Stephens B, Warner SL, Bearss DJ, Vankayalapati H, Sharma S.

J Med Chem. 2013 Dec 12;56(23):9496-508. doi: 10.1021/jm400870h. Epub 2013 Nov 23.

PMID:
24237195

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