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：

新加坡国家研究基金会; 英国医学研究理事会;

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

[1] UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development [J].

Agger, Karl ;

Cloos, Paul A. C. ;

Christensen, Jesper ;

Pasini, Diego ;

Rose, Simon ;

Rappsilber, Juri ;

Issaeva, Irina ;

Canaani, Eli ;

Salcini, Anna Elisabetta ;

Helin, Kristian .

NATURE, 2007, 449 (7163) :731-U10

[2] The H3K27me3 demethylase JMJD3 contributes to the activation of the INK4A-ARF locus in response to oncogene- and stress-induced senescence [J].

Agger, Karl ;

Cloos, Paul A. C. ;

Rudkjaer, Lise ;

Williams, Kristine ;

Andersen, Gitte ;

Christensen, Jesper ;

Helin, Kristian .

GENES & DEVELOPMENT, 2009, 23 (10) :1171-1176

[3] Iron-chelation properties of phenolic acids bearing catechol and galloyl groups [J].

Andjelkovic, M ;

Van Camp, J ;

De Meulenaer, B ;

Depaemelaere, G ;

Socaciu, C ;

Verloo, M ;

Verhe, R .

FOOD CHEMISTRY, 2006, 98 (01) :23-31

[4] Histone demethylase JMJD3 contributes to epigenetic control of INK4a/ARF by oncogenic RAS [J].

Barradas, Marta ;

Anderton, Emma ;

Acosta, Juan Carlos ;

Li, SiDe ;

Banito, Ana ;

Rodriguez-Niedenfuehr, Marc ;

Maertens, Goedele ;

Banck, Michaela ;

Zhou, Ming-Ming ;

Walsh, Martin J. ;

Peters, Gordon ;

Gil, Jesus .

GENES & DEVELOPMENT, 2009, 23 (10) :1177-1182

[5] PLU-1 nuclear protein, which is upregulated in breast cancer, shows restricted expression in normal human adult tissues: A new cancer/testis antigen? [J].

Barrett, A ;

Madsen, B ;

Copier, J ;

Lu, PJ ;

Cooper, L ;

Scibetta, AG ;

Burchell, J ;

Taylor-Papadimitriou, J .

INTERNATIONAL JOURNAL OF CANCER, 2002, 101 (06) :581-588

[6] The complex language of chromatin regulation during transcription [J].

Berger, Shelley L. .

NATURE, 2007, 447 (7143) :407-412

[7] The Histone Demethylases JMJD1A and JMJD2B Are Transcriptional Targets of Hypoxia-inducible Factor HIF [J].

Beyer, Sophie ;

Kristensen, Malene Maag ;

Jensen, Kim Steen ;

Johansen, Jens Vilstrup ;

Staller, Peter .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2008, 283 (52) :36542-36552

[8] Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity [J].

Bi, Xiangdong ;

Lopez, Christina ;

Bacchi, Cyrus J. ;

Rattendi, Donna ;

Woster, Patrick M. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (12) :3229-3232

[9] Structure-function relationships in flavoenzyme-dependent amine oxidations. A comparison of polyamine oxidase and monoamine oxidase. [J].

Binda, C ;

Mattevi, A ;

Edmondson, DE .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (27) :23973-23976

[10] A 30 Å long U-shaped catalytic tunnel in the crystal structure of polyamine oxidase [J].

Binda, C ;

Coda, A ;

Angelini, R ;

Federico, R ;

Ascenzi, P ;

Mattevi, A .

STRUCTURE, 1999, 7 (03) :265-276

← 1 2 3 4 5 6 7 8 9 10 →