Inhibitors of histone demethylases

被引：78

作者：

Lohse, Brian ^{[1
]}

Kristensen, Jesper L. ^{[1
]}

Kristensen, Line H. ^{[1
]}

Agger, Karl ^{[2
,3
]}

Helin, Kristian ^{[2
,3
]}

Gajhede, Michael ^{[1
]}

Clausen, Rasmus P. ^{[1
]}

机构：

[1] Univ Copenhagen, Dept Med Chem, Fac Pharmaceut Sci, DK-2100 Copenhagen, Denmark

[2] Univ Copenhagen, BRIC, DK-2200 Copenhagen, Denmark

[3] Univ Copenhagen, Ctr Epigenet, DK-2200 Copenhagen, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 12期

基金：

英国医学研究理事会; 新加坡国家研究基金会;

关键词：

Histone demethylases; Epigenetics; Inhibitors; HDM; LSD1; HYPOXIA-INDUCIBLE FACTOR; LYSINE-SPECIFIC DEMETHYLASE-1; MECHANISM-BASED INACTIVATOR; DOMAIN-CONTAINING PROTEINS; CRYSTAL-STRUCTURE; STRUCTURAL BASIS; SUBSTRATE-SPECIFICITY; INDUCED SENESCENCE; POLYAMINE OXIDASE; ANDROGEN-RECEPTOR;

D O I：

10.1016/j.bmc.2011.01.046

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：3625 / 3636

页数：12

共 106 条

[81] Solution structure of the SWIRM domain of human histone demethylase LSD1 [J].

Tochio, N ;

Umehara, T ;

Koshiba, S ;

Inoue, M ;

Yabuki, T ;

Aoki, M ;

Seki, E ;

Watanabe, S ;

Tomo, Y ;

Hanada, M ;

Ikari, M ;

Sato, M ;

Terada, T ;

Nagase, T ;

Ohara, O ;

Shirouzu, M ;

Tanaka, A ;

Kigawa, T ;

Yokoyama, S .

STRUCTURE, 2006, 14 (03) :457-468

[82] Histone demethylation by a family of JmjC domain-containing proteins [J].

Tsukada, Y ;

Fang, J ;

Erdjument-Bromage, H ;

Warren, ME ;

Borchers, CH ;

Tempst, P ;

Zhang, Y .

NATURE, 2006, 439 (7078) :811-816

[83] The ARID domain of the H3K4 demethylase RBP2 binds to a DNA CCGCCC motif [J].

Tu, Shengjiang ;

Teng, Yu-Ching ;

Yuan, Chunhua ;

Wu, Ying-Ta ;

Chan, Meng-Yu ;

Cheng, An-Ning ;

Lin, Po-Hsun ;

Juan, Li-Jung ;

Tsai, Ming-Daw .

NATURE STRUCTURAL & MOLECULAR BIOLOGY, 2008, 15 (04) :419-421

[84] Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors [J].

Ueda, Rie ;

Suzuki, Takayoshi ;

Mino, Koshiki ;

Tsumoto, Hiroki ;

Nakagawa, Hidehiko ;

Hasegawa, Makoto ;

Sasaki, Ryuzo ;

Mizukami, Tamio ;

Miyata, Naoki .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2009, 131 (48) :17536-17537

[85] LUMINESCENT OXYGEN CHANNELING IMMUNOASSAY - MEASUREMENT OF PARTICLE BINDING-KINETICS BY CHEMILUMINESCENCE [J].

ULLMAN, EF ;

KIRAKOSSIAN, H ;

SINGH, S ;

WU, ZP ;

IRVIN, BR ;

PEASE, JS ;

SWITCHENKO, AC ;

IRVINE, JD ;

DAFFORN, A ;

SKOLD, CN ;

WAGNER, DB .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (12) :5426-5430

[86] Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer [J].

van Haaften, Gijs ;

Dalgliesh, Gillian L. ;

Davies, Helen ;

Chen, Lina ;

Bignell, Graham ;

Greenman, Chris ;

Edkins, Sarah ;

Hardy, Claire ;

O'Meara, Sarah ;

Teague, Jon ;

Butler, Adam ;

Hinton, Jonathan ;

Latimer, Calli ;

Andrews, Jenny ;

Barthorpe, Syd ;

Beare, Dave ;

Buck, Gemma ;

Campbell, Peter J. ;

Cole, Jennifer ;

Forbes, Simon ;

Jia, Mingming ;

Jones, David ;

Kok, Chai Yin ;

Leroy, Catherine ;

Lin, Meng-Lay ;

McBride, David J. ;

Maddison, Mark ;

Maquire, Simon ;

Mclay, Kirsten ;

Menzies, Andrew ;

Mironenko, Tatiana ;

Mulderrig, Lee ;

Mudie, Laura ;

Pleasance, Erin ;

Shepherd, Rebecca ;

Smith, Raffaella ;

Stebbings, Lucy ;

Stephens, Philip ;

Tang, Gurpreet ;

Tarpey, Patrick S. ;

Turner, Rachel ;

Turrell, Kelly ;

Varian, Jennifer ;

West, Sofie ;

Widaa, Sara ;

Wray, Paul ;

Collins, V. Peter ;

Ichimura, Koichi ;

Law, Simon ;

Wong, John .

NATURE GENETICS, 2009, 41 (05) :521-523

[87] Chromatin remodeling and cancer, part I: covalent histone modifications [J].

Wang, Gang G. ;

Allis, C. David ;

Chi, Ping .

TRENDS IN MOLECULAR MEDICINE, 2007, 13 (09) :363-372

[88] Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD finger [J].

Wang, Gang G. ;

Song, Jikui ;

Wang, Zhanxin ;

Dormann, Holger L. ;

Casadio, Fabio ;

Li, Haitao ;

Luo, Jun-Li ;

Patel, Dinshaw J. ;

Allis, C. David .

NATURE, 2009, 459 (7248) :847-U6

[89] The lysine demethylase LSD1 (KDM1) is required for maintenance of global DNA methylation [J].

Wang, Jing ;

Hevi, Sarah ;

Kurash, Julia K. ;

Lei, Hong ;

Gay, Frederique ;

Bajko, Jeffrey ;

Su, Hui ;

Sun, Weitao ;

Chang, Hua ;

Xu, Guoliang ;

Gaudet, Francois ;

Li, En ;

Chen, Taiping .

NATURE GENETICS, 2009, 41 (01) :125-129

[90]

WANG JK, GENES DEV, V24, P327

← 2 3 4 5 6 7 8 9 10 11 →