Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9

被引：423

作者：

Greiner, D

Bonaldi, T

Eskeland, R

Roemer, E

Imhof, A

机构：

[1] Univ Munich, Histone Modificat Grp, Adolf Butenandt Inst, Dept Mol Biol, D-80336 Munich, Germany

[2] Leibniz Inst Nat Forsch & Infekt Biol, Hans Knoll Inst Nat Forsch, Abt Mol Nat Forsch, D-07745 Jena, Germany

来源：

NATURE CHEMICAL BIOLOGY | 2005年 / 1卷 / 03期

关键词：

D O I：

10.1038/nchembio721

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：

Histone methylation plays a key role in establishing and maintaining stable gene expression patterns during cellular differentiation and embryonic development. Here, we report the characterization of the fungal metabolite chaetocin as the first inhibitor of a lysine-specific histone methyltransferase. Chaetocin is specific for the methyltransferase SU(VAR) 3-9 both in vitro and in vivo and may therefore be used to study heterochromatin-mediated gene repression.

引用

页码：143 / 145

页数：3

共 14 条

[1] The Arabidopsis thaliana genome contains at least 29 active genes encoding SET domain proteins that can be assigned to four evolutionarily conserved classes
Baumbusch, LO
Thorstensen, T
Krauss, V
Fischer, A
Naumann, K
Assalkhou, R
Schulz, I
Reuter, G
Aalen, RB
[J]. NUCLEIC ACIDS RESEARCH, 2001, 29 (21) : 4319 - 4333
[2] A combination of different mass spectroscopic techniques for the analysis of dynamic changes of histone modifications
Bonaldi, T
Imhof, A
Regula, JT
[J]. PROTEOMICS, 2004, 4 (05) : 1382 - 1396
[3] The N-terminus of Drosophila SU(VAR)3-9 mediates dimerization and regulates its methyltransferase activity
Eskeland, R
Czermin, B
Boeke, J
Bonaldi, T
Regula, JT
Imhof, A
[J]. BIOCHEMISTRY, 2004, 43 (12) : 3740 - 3749
[4] Loss of acetylation at Lys16 and trimethylation at Lys20 of histone H4 is a common hallmark of human cancer
Fraga, MF
Ballestar, E
Villar-Garea, A
Boix-Chornet, M
Espada, J
Schotta, G
Bonaldi, T
Haydon, C
Ropero, S
Petrie, K
Iyer, NG
Pérez-Rosado, A
Calvo, E
Lopez, JA
Cano, A
Calasanz, MJ
Colomer, D
Piris, MA
Ahn, N
Imhof, A
Caldas, C
Jenuwein, T
Esteller, M
[J]. NATURE GENETICS, 2005, 37 (04) : 391 - 400
[5] The epipolythiodioxopiperazine (ETP) class of fungal toxins: distribution, mode of action, functions and biosynthesis
Gardiner, DM
Waring, P
Howlett, BJ
[J]. MICROBIOLOGY-SGM, 2005, 151 : 1021 - 1032
[6] Linking the epigenetic 'language' of covalent histone modifications to cancer
Hake, SB
Xiao, A
Allis, CD
[J]. BRITISH JOURNAL OF CANCER, 2004, 90 (04) : 761 - 769
[7] ISOLATION AND STRUCTURE ELUCIDATION OF CHAETOCIN
HAUSER, D
WEBER, HP
SIGG, HP
[J]. HELVETICA CHIMICA ACTA, 1970, 53 (05) : 1061 - &
[8] Translating the histone code
Jenuwein, T
Allis, CD
[J]. SCIENCE, 2001, 293 (5532) : 1074 - 1080
[9] Mei SP, 2004, INT J ONCOL, V25, P1509
[10] Regulation of chromatin structure by site-specific histone H3 methyltransferases
Rea, S
Eisenhaber, F
O'Carroll, N
Strahl, BD
Sun, ZW
Schmid, M
Opravil, S
Mechtler, K
Ponting, CP
Allis, CD
Jenuwein, T
[J]. NATURE, 2000, 406 (6796) : 593 - 599

← 1 2 →